Inhibitory or blocking agents of molecular generating and/or inducing functions

ABSTRACT

A method for inhibiting or blocking molecular generating and/or inducing functions of molecules using an inhibitory or blocking agent of the formula:  
                 
 
     wherein R 1-6  and A are as defined herein.

TECHNICAL FIELD

[0001] This invention relates to compounds which have inhibitory effector blocking effects on substrates (for example, lipids, carbohydrates,amino acids) of less than 10000 of molecular weight which hasconstituted structure and function of organism fundamentally and,function which is generated by macromolecules such as peptides,proteins, enzymes, nucleic acids and genes (DNA, tRNA, mRNA, rRNA) whichare synthesized biologically. These applications of those inhibitoryeffects or blocking effects relate to antibacterial agents, antifungalagent, antiviral agent, bactericidal and/or sterilized agents (foodstuff preserving agents, germination inhibitory or maturation inhibitoryagents for fruits and vegetables, antibacterial agents accompanied withforming or elaborating process of plastics, antimicrobial coatingmaterials and, waxes for interior materials and floor, preventableagents of bacterial and fungal proliferation and/or infection for householding electric instruments, daily use goods, house furnishings and,agents for preventing of bacterial and fungal proliferation and/orinfection for paper and pulp such as slime cleaning agents on industrialfield of electronics, preventable agents of bacterial and fungalproliferation and/or infection for metal processing, preventable agentsof bacterial and fungal proliferation and/or infection for the disposalof wastes), and those are also related to anticancer drugs,contraceptive agents for external use and/or spermatocidal agents,anticoagulants and/or antifibrinolytic agents, modulating agents offunction of bioactive substances and/or inhibitors of bioactivesubstances such as enzymes, peptides, genes and so on, inhibitory and/orblocking agents of antigen-antibody reaction, organ and tissuepreservatives, thrombolytic agents, conformation altering agents ofsaccharide-chains, agents for preventing arteriosclerosis, metabolism(lipids, sugar) improving agents, agents for wound healing,epithelialization promoting agents (including restoration effect ofhair). Moreover, those are related to reductants of non-biologicalmolecules (phospholipids, glyceryl group, sulfudoryl group, thiol estergroup; monosaccharide and disaccharide with polysaccharide, silicone,vinyl, cellulose and so on), free radical scavengers, desulfurizationagents and/or oxidation preventing agents. In addition, those arerelated to the following effects concerning low molecules and/ormacromolecules of non-biological substances, based on chemical andorbital dynamic concept concerning the inhibitory or blocking agents ofmolecular generating and/or inducing functions, which is proposed inthis invention. Those are related to depolymerization agents, improvingagents for surface active substances, phase transition agents, improvingagents of phase transition, plasticity and/or elasticity promotingagents, plasticity and/or elasticity improving agents (plasticizers),fiber flexibility promoters, improving agents for fiber flexibility,glutinous agents, viscidity improving agents, adhesives, adhesiveproperty improving agents, painting agents, improving agents ofpainting, moldability improving agents, improving agents of moldingforming and/or fabrication, copolymerization agents, stabilizers,antioxidants, improving agents for filling and plugging, agents forimproving smoothness, ultraviolet rays absorbents, ultraviolet raysabsorptivity improving agents, shock-resistant improving agents,improving agents for light stability, improving agents of moldlubricants, mold releasing agents, parting agents or surface lubricants,improving agents of molecular ring creator. Moreover, those are relatedto improving agents of wear resistance and/or abrasion resistance, agingresistors and/or durability, improving agents of material property andit's function, fluidability improving agents, improving agents forproperty of water absorption, improving agents for property of waterresistance, improving agents for rigidness, hardness and softness,improving agents of crystallized materials and/or amorphous materials,flexibility promoters, and improving agents for changing flexibility.And, those are related to improving agents of physical property ofmacromolecules composite materials, function improving agents ofmacromolecules composite materials, improving agents of physicalproperty of functional macromolecules composite materials, functionimproving agents of functional macromolecules composite materials,modulation agents and/or improving agents of excitation wavelength andfluorescent wavelength on pigmentums, coating materials, cosmeticpigments, colorants, photolysis agents and improving agents ofphotolysis.

BACKGROUND ART

[0002] Formerly, it has been well known that the basic principle oforganic structural chemistry such as bond angle, molecular weight,acidity, bond length, structure, hydrogen bond, resonance, basicity,optical activity, configuration, and conformation is important as wellas mechanism of chemical reactions (by Morrison and Boyd, organicchemistry, 6th edition, Tokyo Kagaku Doujinn publication at reference<ref. 1>). On the other hand, for example, elements of living organismconsist of lipids, carbohydrates,proteins, enzymes, nucleic acids,macromolecules amino acids and peptides and genes (for example, DNA,tRNA, mRNA, rRNA) and by those elements, in addition, formation of cellmembrane, intracellular organella, intracellular and/or extracellularsubstrates are constructed. Function of these complex substances isgenerated by multi-dimensional structure (conformation) depending oneach substance. In order to understand the mechanism which is related todevelopment and generation of each physiological function (recognitionand/or acceptance of substance), it is important to understand themulti-dimensional structure which each substance has. (Alberts, Bray,Lewis, Raff, Roberts and Watson works, The Molecular Biology of theCELL, Garland Publishing Inc., 3th. edition <ref. 2>). It is also knownthat methyl group contributes in order to produce fluidability andhydrophobicity of substances in the non-living organism, which containslipids, proteins and so on. <ref. 1>. The cell membrane of organism,which is the base units separating from external environment, alsoconsists of hydrophobic component of lipids outside a membrane. And,this cell membrane has important role in signal acceptance into a cellfrom another cell. To connect and adhere between each cell and tosurround intercellular organella also constructed with extremely thinfilm-like membrane which consist of lipids and proteins molecules. Theproteins which is embedded in the membrane has highly biologicalactivities as intermediates around the cell, and between an inside oforganella and cytoplasm. According to types of cells, it is an existenceof various enzymes which involves in intracellular signal transductionand in intercellular respiration. In addition, it is also known thatthere is a substance such as tubulin which is relation on morphologickeep of cell, mitosis and prolifelation. Moreover, proteins in a plasmamembrane contribute to recognize signals between cells. Hydroxyl group,sulfudoryl group (—SH) and disulfide bond are constituted ester.According to these cross-linking reaction, also, physiological functionswhich are generated by multi-dimensional structure of a substance arealtered. In addition, amino nitrogen generates property of basicity aswell as nucleophilic property on molecular reaction. When peptides andproteins are denaturated, coiling of each peptide and proteins isrelaxed; Thus, the particular multi-dimensional structure of the peptideand proteins is crumbled, followed by losing a particular bioactivity ofthe peptides and proteins. Moreover, such change in conformation appearsnot only in peptide and proteins but in complex substance withphospholipids and glycoproteins (for example, nucleic acids). Inaddition, in order to maintain a specificity of each physiologicalfunction which is generated by moiety of membrane, a substance which issecreted into the outside of cells, enzymes which exists into the cell,cytoskeleton and a substrate which is synthesized within cell, it isalso known that it is important that each substance forming livingorganism has two-dimensional and three-dimensional configuration such ashelical structure and sheet. A state of charge distribution and electriccharge density of molecules which consist of substances and is generatedfunction by these multi-dimensional structure differs in speciesdifferences and morbidity <ref. 2>. In addition, virus, which has notcell membrane and is not living organism, consists of peptides chainwhich are constructed by many amino acid bindings. And, these virusparticles have also multi-dimensional structure such as two-dimensionand/or three-dimension. Among multi-dimensional structure, helicalstructure is formed in 3.6 amino acid residues per one helical rotation.Thus, it produces a space which side chain can occupy. And, possiblehydrogen bonds on this helical structure can be constituted all. Inaddition, multi-dimensional structure generates the function of αdomain, beta domain, α/beta domain, exon or intron. This concept is alsoa scientific fact and important knowledge. Though a core part of thisstructure is conserved in homologous proteins, dimensional changes in ahelix loop region occur. Moreover, formation of conformation depends ona type of the secondary structure to bind each loop and a number ofamino acids in helix loop rather than amino acid sequences. Therefore,it is in general to be determined by combination of α—α, beta-beta,α-beta or beta sheet-α loop. And, multi-dimensional structure of helixloop induces a change of cytoskeleton mitosis and prolifelationaccording to change in conformation of each substance (for example,tubulin and spectrin) resulting from changes in an intracellular energy.Moreover, recent scientific topics is to know mechanism of oncogeneis,mechanism of anticancer agents, mechanism of anti-proliferation, naturalcell death (for example apoptosis), mechanism of aging process of thenerve cell, cell recognition or mechanism of cell adhesion. While suchscientific knowledge is turned into basement, it is hoped fordevelopment of new drugs which is utilized to organism such as humanbeing. Though pharmacological effects of conventional antibacterialagents and anticancer drugs have been introduced at cell death, primarymechanism of cell death due to those conventional antibacterial agentsand anticancer drugs is to raise denaturation, coagulation and/ornecrosis. For this reason, an appearance of mutants and resistantstrains as major scientific problems has been left numerously to beresolved. From such a reason, additionally, scientific interest inmechanism of apoptosis arises at present. Moreover, living organism canmove automatically by a flagellum and pilli, and a supermicro-size ofmotor has been provided for pilli of spermatozoa. On driving motor ofthis organism, energy which is generated by hydrolysis of ATP isutilized. A change in this energy produces to alter multi-dimensionalstructure of the helix loop which is configurated by myosin. Thesemulti-dimensional structure is to apply to molecular biology of everykinds of genes and antibodies from recent knowledge. It is well knownscientific fact and knowledge that it is important to generatephysiological function based on recognizing two- or three-dimensionalconformation of each substance <ref. 2>. But, it has been known that thesubstance which consists of living organism does not usually exist in aninitial position and, it exists in dynamic state (for example, movementof membrane proteins is slower than that of lipids molecules which isabout 100 times later). In addition, if movement of lipids moleculeresults in more animation, fluidability of a membrane indeed becomeslarger. But, the speed of the movement differs dependently on types oflipids. A self-action adjustment capability of membrane fluidabilityholds in organism. On the other hand, it is also known that a hindranceof those adjustment capability causes onset of diseases in human being.For this reason, it is hoped standby that the countermeasure is proposedagainst a hindrance of the adjustment capability. In addition,interaction of hydrophobicity between hydrophobic groups is greatlycommitting in stability of lipids bilayer of the biomembrane which isknown as a fluidability model. Moreover, since side chain of many aminoacids with hydrophobic property flanking in an inside of proteins, itdoes not come in contact with to water. For this reason, it is also wellknown that multi-dimensional structure of proteins is kept by hydrogenbond, hydrophobic interaction and van der Waals force and, it makes aflexible matrix. Greater hydrophobic solute is more easily to bind toproteins. In order to get in a hydrophobic region close at proteinssurface which hydrophobic molecule exists, it is thought thatconformation of proteins changes. In this way, when life events isunderstood, it is to be important to understand life activitydynamically and multidimensionally. According to a base of thescientific logic mentioned above, the scientific interest in controllingquality of physiological activity is needless to say and, proposal of anew manner for prevention and treatment of various kinds of diseases iseagerness historically.

[0003] Though it is not necessary to do more than to read history ofrelationship between a man and diseases, a fighting to pathogenicmicrobacterial infection such as bacteria and virus, it is seriousproblems which needs a medical resolution. And, even though developmentof advanced medical technology, it is a serious problem that multipleorgan failure accompanied with sepsis and disseminated intravascularcoagulation causes to result in the death of human being(Hypotension—for clinician to understanding pathophysiology—Fujita Publ.by Koyama) <ref. 3>. Various kinds of pathogenic microbacteria such asstaphylococcus aureus, streptococcus, E. Coli, acid-fast bacteria,mycete and virus usually exist on the living space of human being asorigin of various infectious diseases. Up to this time, sanitatoryadministration to the living space of human being can have been turnedinto prevention of this pathogenic microbacterial and viral infection.Thus, lots of drugs are utilized in a treatment and prevention forinfectious disease in living space of human being, by using disinfectantand/or bactericidal agents. As a result, lots of the fruits have beenraised. However, while development of antibacterial agents isnoticeable, application of drugs concurs at an appearance of a resistantstrain and, a social administrative problem as well as difficulties ofmedical care has been raised. For example, it is an appearance ofvarious kinds of multi-drug resistant strains which represent methitilinresistance staphylococcus aureus (<MRSA> with abbreviation). In order toshow resistance to lots of beta-lactam group drugs in staphylococcusaureus, a treatment for infectious disease due to MRSA is difficult and,it becomes pathogenic organism such as opportunistic infection andpostoperative infection in clinical practices and, an infected patientto this MRSA changes a serious illness and, he is easy to fall intosepsis and multiple organ failure. Thus, onset of untreatable infectiondue to MRSA is a serious social issue. An infection of pseudomonasaeruginosa is anxious for preventing secondary infection from burninjury as a complication. From a point of related view with cysticpulmonary fibrosis, recently, an approach to preventing this infectionof pseudomonas aeruginosa is a great problem. Moreover, many interestsare recently brought nearer to helicobacter pylori as a cause of pepticulcer or abhorrent factor. In addition, infection of acid-fast bacteriaand mycete is international problems as for an infectious complicationwhose acquired immune deficient syndrome (AIDS) is fatal. Therefore, itis an important international request that it is developed valid drugson an infectious disease by virus, drugs which have potencies ofantimicrobacterial effect to MRSA and/or acid-fast bacteria, drugs forE. Coli which is easy to cause sepsis, drugs which have potencies ofantifungal effect.

[0004] And also, recently, opportunistic infection in daily living space(for example, air-conditioning contamination according to regionerae)and on surrounding in life behavior as well as in a hospital becomeserious problems and, bactericidal and/or sterilized agents isrecognized again as a prevention countermeasure of bacteriacontamination including opportunistic infection. An appearance ofsociety which is populated by many aged generation has been appealed inthe near future and, urgent technological development is expected acounterattack of medical care for the aged.

[0005] Generally, staphylococcus aureus, acid-fast bacteria, mycete andvirus are easy to encounter an opportunity of an infection throughrespiratory system such as nasal cavity and pharynx, and throughdigestive tract. Conventional bactericidal and/or sterilized agentsfrequently depends on a physical manner by living space of human beingand at surroundings in life behavior and, moreover, major administrationroute of drugs such as antibiotic is sometimes restricted in the way oforal administration, intravenous administration and/or directadministration to the infection focus and, there is some apprehensionsand inconveniences to medical care specialists, a nursing volunteers andhome helpers as well as patients them self. But, during a period whichpeople is alive, we have to continue to come in contact with an externalair through skin and respiratory system. Thus, it is expected to utilizeroom air which is living space, for preventing or treating infectiousdiseases. Generally, in order that bacteria can obtain their resistantabilities by various genetic mechanism such as mutation, selection,character introduction, autotransduction of plasmid, bacterial infectioncan not be prevented completely by using of conventional simplesubstance which is chemically synthesized and, the chemotherapeuticagents without induction of being a resistant strain also have notsupplied until the present. And, as an aim for an inhibition of aprimary structure of the substances which consist of bacterial membrane,a few of drugs with antimicrobacterial effect has been appliedabundantly. All the more, while developments of an administration mannerof antibacterial agents are also important and are anticipated,additional development of new antibacterial, antifungal agents and/orand antiviral agents which affect on multi-dimensional structure isexpected strongly. Moreover, for a marked increase in population on theearth, namely developing countries, it is important to propose apossible planning of birth control even in regarding with supplyingfoods and trusting of natural resource in the future. However, though ause of physical contraception such as condom and pessary is as a matterof course as for planning of birth control, ovulation control by use ofa female sex hormone and operative contraception to both male and femaleis driven proposal internationally. In order to avoid to be damaged theheredity information of spermatozoa to suppress it's fertility, a newmethod of the contraception which can inhibit a movement ability ofspermatozoa is also expected. On the other hand, in order to generatethe function of living organism, multi-dimensional structure ofsubstances as above-mentioned plays an important role. However, thoughit is expected that a substance with simple chemical structure caninhibit and/or block the function generated or induced by themulti-dimensional structure of biological substances, there is notproposal of such representative substance, which is little harm andsafety, concerning life continuation as integrated whole body at thepresent. Not only proposal of such representative substances and severalproofed efficiencies above mentioned is interest in academic events suchas biology, chemistry and medicine, but it is sought that such asuggestion is hastily proposal in practical medical care.

[0006] Numerous daily materials, industrial and environmental materialsare provided to develop at the present society by understanding,analyzing, manufacturing and improving physical property of low moleculesubstances and macromolecules substances and by utilizing theirfunctional properties. But, by qualitatively advancing improvement ofphysical property of low molecule substances and macromoleculessubstances, an expectation is to propose a representative which makesfunction, efficiency, comfortableness and safety. For example, physicalproperty of a macromolecules substance such as surface activitysubstance and polymerization substance is described briefly.

[0007] A magnitude of surface activity relates on criticality densityfor micell formation and solubilization. And, Krafft point is lower as achain-like (rod-like) part with the substance is short. It is knownthat-a value of criticality density of micell formation is greater as achain-like (rod-like) part with the substance is short. According toeach characteristic configuration of molecule in surface-active agentsand/or surfactants, it can effectively produces bubbling formation,wetting, a fall of surface tension, emulsification (formation ofemulsion ), solubilization, formation of micelle detergency. Inaddition, in a case of substance with properties of water insoluble andstrong hydrophilic, a less intermolecular force between it's moleculeand broad wide spreading on the water surface, it is also known that amembrane with one molecular layer (single molecular film) is formed. Ifthis single molecular film can be transferred on the surface of solid, asurface of hydrophobicity is obtained. For this reason, proposal ofimproving agents for surface active substances is that it is prospectedin making thin film such as LB membrane. In addition, surface-activeagents and/or surfactants has a potency of disinfection, stability inhard water. By utilizing these effect, surface-active agents and/orsurfactants are blended cosmetics, cleansing creams, shampoos and rinsesand, they are widely utilized in electrically charging preventive agents(antistatic agents) of plastics and fibers, softening agents of fibers,foaming, frothing, lathering or whipping agents of aerosol and tinctionassistants. Thus, proposal of improving agents for surface activesubstances is prospected in many fields. Moreover, polyethylene isrepresentative in various kinds of polymers. Polyethylene is athermoplastic crystal which is repeated of —CH₂CH₂— and, it producesbranches dependently on a manufacturing method resulting in decrease incrystallinity and rigidity as well as increase in transparence. Inaddition, polyethylene is added short chained branch (for example, ethylbranch and butyl branch) by pull out reaction (abstraction reaction) ofhydrogen within molecule due to back-biting during polymerizationresulting in low density and, branch (long chained branch) which isidentical to main chain of the polymer is produced by pull out reaction(abstraction reaction) of hydrogen between molecules. Linearpolyethylene (LLD polyethylene) has an intensity for impact force. Inaddition, medium density polyethylene (MD polyethylene) and ultra-lowdensity polyethylene (VLD polyethylene) are used as improving orreforming agents of resins. Ultrahigh molecule weight polyethylene (UHMWpolyethylene) is applied widely by the reason that it is superior toself-lubricating, shock resistance and wear resistance and/or abrasionresistance. In this way, it is expected to propose improving agentswhich can approve property of each substance in order to make arise aquality of macromolecules substances. Moreover, each polymer inmacromolecules substances has a characteristic property itself. Forexample, ethylene/vinyl acetate copolymer is superior in springiness,elasticity, transparence, stout and heat seal. Polymer in methacrylicacid ester group among methacrylate resins and resins in acrylonitrilegroup is named generically with metacrylate resin and, they have widelyutilized in materials for illumination, commercial advertising panel,car and train, electrical and/or optic materials, daily goods and so onby use of their superior properties such as surface luster, transparenceand weather resistance. In addition, other physical properties ofpolymers is filmed-formation property, rubber-like property, mechanicalstout, anti-creep, flexibility, thermoplasticity, thermal resistance,dimensional stability, phase transition, shock resistance, fluidability,surface luster, water resisting property and chemical resistance.Moreover, there are processability, printing, painting, deposition,secondary processing such as lamination, epibole, waterproof,separating, bubble-breaking, oxidation prevention, increasing viscosity,pyrogenetically consolidating property, gelatinization at ordinarytemperature, thermal displacement, thermal resistance, alkaliresistance, flexural strength, bending elasticity, tug strength,electric characteristics, adhesion, erosion- or rust-resistance, slidingproperty with thermal resistance, radiation resistance, poly-valencedmetal ion capture ability (chelate ability), dispersibility, aggregationability as another physical properties. Concerning our present socialcivilization life, these macromolecules substances are necessary andindispensable in our daily life. Thus, it is expected to provide moreeffective materials which are improved each physical property bycombining with each physical property. Polyethylene glycol is oneexample of the macromolecules which is daily used in general.Application of polyethylene glycol is widely expanded into themanufacturing fields such as cream lotion in cosmetic industry,lubricant in metal processing and/or fiber industry, binder of tabletfor pills in pharmaceutic industry and basic material for producingsurface-active agents and/or surfactants and, moreover, it is alsoutilized flocculant for inorganic substances such as clay, resin reformagents (prohydration), thickeners, binders for ceramic, pulp dispersingagents and flocculants for pulp. Then, it is expected to be improvedphysical property of polyethylene glycol as more safety and effectivematerials. Moreover, highly polymerized sodium polyethylene acrylic acidis permitted legally as food additive and/or cosmetics material. Thus,it is expected that a proposal of new technique and/or new substance canimprove a physical property resulting from change in multi-dimensionalstructure (conformation) of this polyethylene acryl amide polymer.

[0008] In generating property of various types of fibers such as naturalfibers in cellulose group, synthetic fibers in hydrocarbon group,synthetic fibers in polyvinyl alcohol group, acrylic synthetic fibers,polyamide synthetic fibers, aramide fibers, synthetic fibers inpolyester group, fibers in polyurethane group and carbon fibers, eachcharacteristic feature of those fibers is produced by their moleculeconfiguration and their multi-dimensional structure. Moreover, eachphysical property of natural gum and synthetic rubber latex, which canproduce rubber-like elasticity dependently on given temperature, is alsochanged by alteration of multi-dimensional structure. Collagen alsotakes three pairs of right winding spiral structure resulting fromformation of left winding helix. Thus, the role of function of thiscollagen also differs by it's multi-dimensional structure. Generation offunction corresponding to the aim and it's utilization is also expectedby improving the multi-dimensional structure of collagen fibers.

[0009] Moreover, there are cosmetic pigments, agents in water-solublecoating materials, scale preventing agents, electroconductive treatingagents, stabilizers for emulsion and polymerization, coating materialsutilized paint film formation, coating materials of powder, coatingmaterials for radiation consolidation, soluble non-dispersing coatingmaterials and others as another uses of macromolecules. Those are alsoapplied to housing materials, electricity products, motor vehicles,construction materials, furnitures and electric wire insulation mantlesand so on. From such reasons, proposal of a new technique and/or a newsubstance to improve the physical property of these coating materials isprospected.

[0010] So, in order to extend utilization of macromolecules, appropriateadhesives is also necessary. To improve function of these adhesives andto efficiently utilize macromolecules substances is expected in variousfields such as medical care system, transport system, communicationsystem and constructions.

[0011] Moreover, composite materials of macromolecules with specificfunction is used. The specific function is optical transfer, polarity,recording medium for electronic machines, separating membrane,electrical conductivity, electrical conductivity with transparence,electricity conductivity related to optical radiation,vibration-damping, sound arresting, heat conductivity and so on.Additionally, composite materials of macromolecules with specificfunction has a possible potential to apply into tip materials such asmodule for separation, metallizing resins, impact-relaxation materials,vibration-damping conductive materials, optic fibers, magnetic recordingmedium, optical recording medium, rewritable optical disc. For thisreason, a new technique and possible idea which can easily control thefunction of composite materials as well as change in configuration ofthe materials are expected in order to make function and performancebetter.

[0012] In addition, functional polymers which can cause a chemicalchange or a physical change by physical and chemical stimuli externallyand which can produce a state change by interaction with a correspondingsubstance are generated by effects of reactable substrate with specificfunction which is introduced into main chains and/or side chains ofmacromolecules or it's precursor and by a proportional property andspecific conformation of an additive. For example, there are materialsfor electricity, semiconductor related materials, photosensitivepolymeric materials, recording materials, materials for liquid crystaldisplay, tip materials, liquid crystal materials of macromolecules,optoelectronics materials, materials for thin films, photochromicmaterials, optical recording materials, optical tip materials,holographic recording materials, nonlinear optical tip materials,optical responding materials, sensor related materials and transducerrelated materials as functional polymer composites. Therefore, in orderto make well generation, good efficiency and accurate stabilization ofeach functional property, it is expected to improve function of thesepolymers. In addition, an improvement of printed circuit board materialsfor the optical disc which needs property such as transparence,mechanical intensity and thermal resistance and of thin film materialssuch as the amorphic membrane which polymerized membrane is cross-linkedtridimensionality is also expected. Moreover, as an applied example ofmacromolecules, there is also polymer with photochemistry reaction whichcauses a configuration change such as cross-linking, polymerization,polarity change, decomposition and depolymerization due to light. Thus,as well as improvement of chemical structure of these photosensitivefunctional polymers, it is also expected that proposal of a newtechnique and possible idea which can improve a physical property ofmaterials by changing those conformation.

[0013] Moreover, there are also macromolecular substances which havebeen utilized for detergents, cosmetics and foodstuff. A substance withmore useful physical property which results from improving conformationaccompanied with generating functional property has been expected tomake quality of life and environment better. Additionally, property ofmacromolecules is utilized as supporting materials in medical healthcare, then, it is also expected to propose useful and new biomaterialswhich have better fitness and adaptation to body by improving propertyof conventional biomaterials which is utilized macromolecules. Inaddition, there are also stabilizers which makes stability against heatand light, antioxidants (age resistors) which prevents progress ofoxidation and ozonolysis, promoting agents which makes plasticity,elasticity and processability well and softener. Moreover, there arealso flame retarders with fire-resistance, cross-linking agents,fillers, treating agents for fibers, oily agents, electrically chargingpreventive agents (antistatic agents), final forming agents forflexibility, final forming agents for polymers, additives for plastics,ultraviolet rays absorbents, optical stabilizers, lubricants, curingagents and/or vulcanizing agents, age resistors and softeners. Inaddition, there are also sclerosing agents and tackifiers, reinforcers,fillers, additives for adhesives, additives for coating materials,cosmetic pigments, solvents, consolidation accelerators, deteriorationpreventives, dispersing agents as a tool as additives of polymericmaterials. Then, it is known well that those are used corresponding toeach objective. By improving property of such additives which are usedfor these polymeric materials, it is expected to provide a new materialwhich has useful functional property.

[0014] Moreover, there are various kind of macromolecules for using asdetergents, cosmetics and foodstuff. Macromolecules in foodstuff as anexample are representative substances such as polysaccharides, foodstuffproteins and macromolecules for gum. Macromolecules for gum, forexample, have natural resins such as chicle, soruba and jelutong whichcontains polyethylene isoprene and which is utilized chewing gum asnatural additives. In addition, there are vinyl acetate resin,polyisobutylene, polyethylene butene, isobutylene-isoprene rubber,styrene-butadiene rubber (SBR), polyethylene, terpene resin and so on asfood additives. Macromolecules extracted from plants and/or animals aswell as synthesized macromolecules are used in detergents and cosmetics.Thus, it is important that in the point of view at better quality oflife itself as well as life space, physical property of macromolecularsubstances is improved it's conformation generating specificcharacteristic and function,resulting in being useful one. In addition,an example of utilizing a property of macromolecules as medical careaids materials is a dialysis membrane. As a material of a dialysismembrane, though natural macromolecules (celluloses, cellulose-acetatefibers) and synthesized macromolecules (for example,polymethylmethacrylate, polyacrylonitrile, polysulfone, ethylene/vinylalcohol copolymer) is general purposed, it is also expected to develop auseful and well adapting biomaterials by improving property of theseconventional biomaterials. Moreover, prospected additives areantioxidants (or age resistors) which prevent an progress of oxidationand ozonolysis and stabilizers which make stability constant againstheat and light. It is also expected to make each performance better byprocessing a new additive to promoting agents which makes plasticityand/or elasticity, softeners, flame retarders which is addedflame-resisting, cross-linking agents (or curing agents and/orvulcanizing agents), fillers, treating agents for fibers, oily agents(for example, spinning oil), antistatic agent (for example, compoundswith polyethylene glycol chain, surface-active agents and/orsurfactants), final forming agents for flexibility, final forming agentsfor polymers or additives for plastics. Ultraviolet rays absorbents,optical stabilizers, lubricants, curing agents and/or vulcanizingagents, and age resistors are also important as additives. Softener hasan effect as a lubricant in the intermolecular space of gum and has apotency of controlling dispersibility of other additives and, they playa role of increasing in volume of combination agents. In order toproduce better physical property such as hardness, tug strength,modulus, anti-elasticity, friction resistance, wear resistance, tearresistance into carbon black and rubber goods, tackifiers and/orreinforcers frequently are added. In addition, fillers, additives foradhesives, additives for coating materials, cosmetic pigments, solvents,sclerosing agents, consolidation accelerators, deteriorationpreventives, dispersing agents and so on are used as additives ofmacromolecular materials according to each objective. It is expected toimprove property of those additives for various kinds of macromolecularmaterials as above mentioned.

[0015] In conformity with a biological fact mentioned above, it isexpected to provide a representative agent and/or drug with thefollowing effects, that can inhibit or block the function generated bymulti-dimensional structure of substances which consists of livingorganism; extracellular matrix, cell membrane, cytoskeleton, cytoplasmand components of intracellular organella such as enzymes, genes,antibody, proteins, sugars, lipids. Those agents and/or drugs areantibacterial agents, antifungal agent, antiviral agent, bactericidaland/or sterilized agents, anticancer drugs, anticoagulants and/orantifibrinolytic agents, blood coagulation and fibrinolysis blockingagents, inhibitory and/or,blocking agents of antigen-antibody reaction,organ and/or tissue preservatives, food preservatives. In addition,those agents and/or drugs are also germination or maturation inhibitoryagents of fruits and vegetables, antibacterial agents for plasticprocessing, antimicrobial coating materials, antimicrobial resin waxes,house holding electric instruments, agents for preventing of bacterialand fungal proliferation and/or infection of house furnishings and dailyuse goods, slime preventing agents for pulp and paper, cleaning agentson field of electronics, agents for preventing bacterial and fungalproliferation and/or infection on metal processing oil (metal workingfluid), the agents for preventing bacterial and fungal proliferationand/or infection on the disposal of waste. Moreover, it was hoped fordevelopment of inhibitory agents and/or blocking agents of function dueto bioactive substances such as enzymes, peptides and genes,spermatocidal agents or contraceptive agents for external use,thrombolytic agents, conformation altering agents of saccharide-chains,agents for preventing arteriosclerosis, metabolism (lipids, sugar,proteins) improving agents, agents for wound healing, epithelializationpromoting agents, and inhibitors and/or blocking agents which are ableto inhibit or block function generated by the multi-dimensionalstructure of substance which living organism has many kinds ofsubstrates.

[0016] Objective of this invention is to resolve problems abovementioned, and is to provide inhibitory or blocking agents of moleculargenerating and/or inducing functions, that can inhibit or block functiongenerated by multi-dimensional structure of reactive substrates and hasa simple chemical structure.

DISCLOSURE OF THE INVENTION

[0017] In order to complete above-mentioned objective, as the resultthat the inventors repeated research with all our mind, this inventioncame to be completed that the chemical compounds which is shown in thefollowing general formula (1-a) (1-b), general formula (2), generalformula (3-a) (3-b) or those acid addition salt compounds which areactive provide the objective mentioned above.

[0018] The invention mentioned on claims 1-4 in order to completeabove-mentioned objective is the inhibitory or blocking agents ofmolecular generating and/or inducing functions which has the originalmolecular structure shown in general formula (1-a) (1-b). And, thecompounds, the derivatives or those acid addition salt compounds provideantibacterial agents, antifungal agent, antiviral agent, bactericidaland/or sterilized agents, anticancer drugs, blood coagulation andfibrinolysis inhibitors and/or blocking agents, inhibitory and/orblocking agents of antigen-antibody reaction, organ and/or tissuepreservatives, antiseptics and preservatives for foodstuffs, germinationand maturation inhibitory agents for fruits and vegetables. In addition,the compounds, the derivatives or those acid addition salt compoundsprovide antibacterial agents for plastic processing, antimicrobialcoating materials, antimicrobial resin waxes, agents for preventing ofbacterial and fungal proliferation and/or infection of house holdingelectric instruments, daily use goods and house furnishings, slimepreventing agents for papers and pulps, cleaning agents in field ofelectronics, agents for preventing bacterial and fungal proliferationand/or infection for metal processing oil (metal working fluid), agentsfor preventing bacterial and fungal proliferation and/or infection forthe disposal of waste. In addition, the compounds, the derivatives orthose acid addition salt compounds provide spermatocidal agents and/orcontraceptive agents which aim to suppress fertility of spermatozoa,thrombolytic agents, conformation altering agents of saccharide-chains,agents for preventing arteriosclerosis, metabolism (lipids, sugar)improving agents, agents for wound healing, epithelialization promotingagents (including hair restoration effect), inhibitors and/or blockingagents which can control generation of function with bioactivesubstances (for example, enzymes, peptides, gene). In addition, thecompounds, the derivatives or those acid addition salt compounds caninhibit and/or block function generated by multi-dimensional structure(conformation) of the substance which consist of a shape and function ofliving organism. Moreover, the compounds, the derivatives or those acidaddition salt compounds-provide chemical substances which can control,inhibit and/or block the function which is generated bymulti-dimensional structure (conformation) with macromoleculessubstances and macromolecules composite materials as well as livingorganism. In addition, when halogen compounds such as halogenated alkalimetals or halogenated alkali-earthy metals or halogenated zinc is addedin the compounds which were provided by this invention, a reaction isable to be induced. Moreover, when gold colloid is added in thecompounds which were provided by this invention, marking and/or labelingsubstances can be made and, it is also possible to use the compoundswhich were provided by this invention as dispersion (diffusion)preventives of tinction and printing dye, ink stabilizers or dyesticking agents. In addition, by using a color coupler such as dye withthe compounds which were provided by this invention, coloring of the dyecan be enhanced. When fragrant agents is used with the compounds whichwere provided by this invention, possible fragrance can be produced. Inaddition, the compounds, the derivatives or those acid addition saltcompounds can be utilized as depolymerization agents, surface-activeagents and/or surfactants, improving agents for surface activesubstances, phase transition agents, improving agents of phasetransition, improving agents of microphase separation structure,plasticity and/or elasticity promoting agents, plasticity and/orelasticity improving agents (plasticizers), copolymerization agents,copolymerization improving agents, improving agents of fluorescentwavelength of colorants, polymerization regulators, improving agents ofpolymerization adjustment, stabilizers, stabilization improving agents,antioxidants, oxidation preventing agents, agents for improvingcrystallized materials and/or amorphous materials, fluidabilityimproving agents, flexibility promoters, improving agents for changingflexibility, alterable agents of excitation wavelength, fluorescentwavelength and excitation wavelength of pigmentums, coating materialsand cosmetic pigments. And, it is also possible to utilize thecompounds, the derivatives or those acid addition salt compounds as thefollowing improving agents, Those are agents which can improve physicalproperty of low molecule substances, agents which can improve functionof low molecule substances, agents which can improve physical propertyof macromolecules substance, agents which can improve function ofmacromolecules substances, and agents which can improve physicalproperty of macromolecules composite materials and functionalmacromolecules composite materials.

[0019] However, in the formula,

[0020] (i) R1, R2, R3, R4, R5, R6, R10 and R11 represents independentlyhydrogen atom; halogen atom; C1-C6 alkyl group; amidino group; C3-C8cycloalkyl group; C1-C6 alkoxy C1-C6 alkyl group; aryl group; allylgroup; aralkyl group in which one or more C1-C6 alkyl groups are boundto an aromatic ring selected from the group consisting of benzene,naphthalene and anthracene ring; C1-C6 alkylene group; benzoyl group;cinnamyl group; cinnamoyl group or furoyl group;

[0021] (ii) A represents hydrogen atom or

[0022] (wherein

[0023] R7 represents C1-C6 alkyl group; sulfide group or phosphategroup;

[0024] R8 and R9 represent independently hydrogen atom; halogen atom;straight or branched C1-C6 alkyl group; aryl group; allyl group; aralkylgroup in which one or more C1-C6 alkyl groups are bound to an aromaticring selected from the group consisting of benzene, naphthalene andanthracene ring; C1-C6 alkylene group; benzoyl group; cinnamyl group;cinnamoyl group or furoyl group;

[0025] (iii) one or more of R1, R2, R3 and R4, and/or one or more of R5,R6, R10 and R11 may be substituted or non-substituted cyclopentyl group;substituted or non-substituted cyclohexyl group; or substituted ornon-substituted naphthyl group;

[0026] (iv) R5, R6, R10 and R11 may form a ring by binding with anothercondensation polycyclic hydrocarbon compound or heterocyclic compound;

[0027] (v) one or more of R3, R4, R5, R6, R10 and R11 may be substitutedby one or more of substituents selected from the group consisting ofhalogen atom, cyano group, protected or non-protected carboxyl group,protected-or non-protected hydroxyl group, protected or non-protectedamino group, C1-C6 alkyl group, C1-C6 alkoxy group, C1-C7 alkoxycarbonyl group, aryl group, C3-C6 cycloalkyl group, C1-C6 acylaminogroup, C1-C6 acyloxy group, C2-C6 alkenyl-group, C1-C6 trihalogenoalkylgroup, C1-C6 alkylamino group, and C1-C6 dialkylamino group;

[0028] (vi) R2 and/or R5 may be substituted by one or more substituentsselected-from the group consisting of halogen atom, C1-C6 alkyl group,protected or non-protected carboxyl group, protected or non-protectedhydroxyl group, protected or non-protected amino group, protected ornon-protected C1-C6 alkylamino group, protected or non-protected C1-C6aminoalkyl group, protected or non-protected C1-C6 alkylamino C1-C6alkyl group, protected or non-protected hydroxyalkyl group, and C3-C6cycloalkylamino group;

[0029] (vii) when one or more of R3, R4, R5,, R6, R10 and R11 are alkylgroups, terminal end(s) of the alkyl group(s) may be substituted byC3-C8 cycloalkyl group).

[0030] The aryl group in (i), (ii) and (v) may be phenyl, tollyl, xylylor naphthyl group. The substituted cyclopentyl group in (iii) may becyclopentylamino group or cyclopentylcarbinol group, the substitutedcyclohexyl group in (iii) may be cyclohexylamino group,cyclohexylaldehyde group or cyclohexyl acetic acid group, and thesubstituted naphthyl group in (iii) may be naphthylamino group ornaphthylamino sulfonic acid group. The condensation polycyclichydrocarbon compound in (iv) may be pentalene, indene, naphthalene,azulene, heptalene, biphenylene, indacene, acenaphthylene, fluorene,phenalene, phenanthrene, anthracene, pentacene, hexacene,dibenzophenanthrene, 1H-cyclopentacyclooctene or benzocyclooctene, andthe heterocyclic compound may be furan, thiophene, pyrrole, γ-pyran,γ-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole orquinoline.

[0031] The invention mentioned on claims 5 and 6 in order to completeabove-mentioned objective is the inhibitory or blocking agents ofmolecular generating and/or inducing function which has the originalmolecular structure shown in general formula (2). And, the compounds,the derivatives or those acid addition salt compounds with effectiveintegents provide antibacterial agents, antifungal agent, antiviralagent, bactericidal and/or sterilized agents, anticancer drugs, bloodcoagulation and fibrinolysis inhibitors and/or blocking agents,inhibitory and/or blocking agents of antigen-antibody reaction, organand/or tissue preservatives, antiseptics and preservatives forfoodstuffs, germination and/or maturation inhibitory agents for fruitsand vegetables, antibacterial agents for plastic processing,antimicrobial coating materials, antimicrobial resin waxes, agents forpreventing of bacterial and fungal proliferation and/or infection ofhouse holding electric instruments, daily use goods and housefurnishings, slime preventing agents for papers and pulps, cleaningagents in field of electronics, agents for preventing bacterial andfungal proliferation and/or infection for metal processing oil (metalworking fluid), agents for preventing bacterial and fungal proliferationand/or infection for the disposal of waste, spermatocidal agents and/orcontraceptive agents which aim to suppress fertility of spermatozoa,thrombolytic agents, conformation altering agents of saccharide-chains,agents for preventing arteriosclerosis, metabolism (lipids, sugar)improving agents, agents for wound healing, epithelialization promotingagents (including hair restoration effect), inhibitors and/or blockingagents which can control generation of function with bioactivesubstances (for example, enzymes, peptides, genes). In addition, thecompounds, the derivatives or those acid addition salt compounds witheffective integents can inhibit and/or block function generated bymulti-dimensional structure (conformation) of the substance whichconsist of a shape and function of living organism. Moreover, thecompounds, the derivatives or those acid addition salt compounds witheffective integents provide chemical substances which can control,inhibit and/or block the function which is generated bymulti-dimensional structure (conformation) with macromoleculessubstances and macromolecules composite materials as well as livingorganism. In addition, when halogen compounds such as halogenated alkalimetals or halogenated alkali-earthy metals or halogenated zinc is addedin the compounds which were provided by this invention, a reaction isable to be induced. Moreover, when gold colloid is added in thecompounds which were provided by this invention, marking and/or labelingsubstances can be made and, it is also possible to use the compoundswhich were provided by this invention as dispersion (diffusion)preventives of tinction and printing dye, ink stabilizers or dyesticking agents. In addition, by using together a color coupler such asdye with the compounds which were provided in this invention, coloringof the dye can be enhanced. When fragrant agents is used with thecompounds which were provided by this invention, possible fragrance canbe produced. In addition, the compounds, the derivatives or those acidaddition salt compounds can be utilized as depolymerization agents,surface-active agents and/or surfactants, improving agents for surfaceactive substances, phase transition agents, improving agents of phasetransition, improving agents of microphase separation structure,plasticity and/or elasticity promoting agents, plasticity and/orelasticity improving agents (plasticizers), copolymerization agents,copolymerization improving agents, polymerization regulators, improvingagents of polymerization adjustment, stabilizers, stabilizationimproving agents, antioxidants, oxidation preventing agents, improvingagents of crystallized materials and/or amorphous materials,fluidability improving agents, flexibility promoters, improving agentsfor changing flexibility, improving agents of fluorescent wavelength andexcitation wavelength of pigmentums, coating materials, cosmeticpigments and colorants, modulating agents of excitation wavelength andfluorescent wavelength of pigmentums, coating materials, cosmeticpigments and colorants. And, it is also possible to utilize thecompounds, the derivatives or those acid addition salt compounds as thefollowing improving agents. Those are agents which can improve physicalproperty of low molecule substances, agents which can improve functionof low molecule substances, agents which can improve physical propertyof macromolecules substance, agents which can improve function ofmacromolecules substances, agents which can improve physical property ofmacromolecules composite materials and functional macromoleculescomposite materials.

[0032] wherein

[0033] (i) R1, R2, R3, R4, R5 and R6 represent independently hydrogenatom; halogen atom; C1-C6 alkyl group; amidino group; C3-C8 cycloalkylgroup; C1-C6 alkoxy C1-C6 alkyl group; aryl group; allyl group; aralkylgroup in which one or more C1-C6 alkyl groups are bound to an aromaticring selected from the group consisting of benzene, naphthalene andanthracene ring; C1-C6 alkylene group; benzoyl group; cinnamyl group;cinnamoyl group or furoyl group;

[0034] (ii) one or more of R1, R2, R3 and R4, and/or one or more of R5and R6 may be substituted or non-substituted cyclopentyl group;substituted or non-substituted cyclohexyl group; or substituted ornon-substituted naphthyl group;

[0035] (iii) R5 and R6 may form a ring by binding with anothercondensation polycyclic hydrocarbon compound or heterocyclic compound;

[0036] (iv) one or more of R3, R4, R5 and R6 may be substituted by oneor more of substituents selected from the group consisting of halogenatom, cyano group, protected or non-protected carboxyl group, protectedor non-protected hydroxyl group, protected or non-protected amino group,C1-C6 alkyl group, C1-C6 alkoxy group, C1-C7 alkoxy carbonyl group, arylgroup, C3-C6 cycloalkyl group, C1-C6 acylamino group, C1-C6 acyloxygroup, C2-C6 alkenyl group, C1-C6 trihalogenoalkyl group, C1-C6alkylamino group, and C1-C6 dialkylamino group;

[0037] (v) R2 and/or R5 may be substituted by one or more substituentsselected from the group consisting of halogen atom, C1-C6 alkyl group,protected or non-protected carboxyl group, protected or non-protectedhydroxyl group, protected or non-protected amino group, protected ornon-protected C1-C6 alkylamino group, protected or non-protected C1-C6aminoalkyl group, protected or non-protected C1-C6 alkylamino C1-C6alkyl group, protected or non-protected hydroxyalkyl group, and C3-C6cycloalkylamino group;

[0038] (vi) when one or more of R3, R4, R5 and R6 are alkyl groups,terminal end(s) of the alkyl group(s) may be substituted by C3-C8cycloalkyl group).

[0039] The aryl group in (i) and (iv) may be phenyl, tollyl, xylyl ornaphthyl group. The-substituted cyclopentyl group in (ii) may becyclopentylamino group or cyclopentylcarbinol group, the substitutedcyclohexyl group in (ii) may be cyclohexylamino group,cyclohexylaldehyde group or cyclohexyl acetic acid group, and thesubstituted naphthyl group in (ii) may be naphthylamino group ornaphthylamino sulfonic acid group. The condensation polycyclichydrocarbon compound in (iii) may be pentalene, indene, naphthalene,azulene, heptalene, biphenylene, indacene, acenaphthylene, fluorene,phenalene, phenanthrene, anthracene, pentacene, hexacene,dibenzophenanthrene, 1H-cyclopentacyclooctene or benzocyclooctene, andthe heterocyclic compound may be furan, thiophene, pyrrole, γ-pyran,γ-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole orquinoline.

[0040] The invention mentioned on claims 7-11 in order to completeabove-mentioned objective is the inhibitory or blocking agents ofmolecular generating and/or inducing functions which has the originalmolecular structure shown in general formula (3-a) (3-b). And, thecompounds, the derivatives or those acid addition salt compounds witheffective integents provide antibacterial agents, antifungal agent,antiviral agent, bactericidal and/or sterilized agents, anticancerdrugs, blood coagulation and fibrinolysis inhibitors and/or blockingagents, inhibitory and/or blocking agents of antigen-antibody reaction,organ and/or tissue preservatives, antiseptics and preservatives forfoodstuffs, germination and/or maturation inhibitory agents for fruitsand vegetables, antibacterial agents for plastic processing,antimicrobial coating materials, antimicrobial resin waxes, agents forpreventing of bacterial and fungal proliferation and/or infection ofhouse holding electric instruments, daily use goods and housefurnishings, slime preventing agents for papers and pulps, cleaningagents in field of electronics, agents for preventing bacterial andfungal proliferation and/or infection for metal processing oil (metalworking fluid), agents for preventing bacterial and fungal proliferationand/or infection for the disposal of waste, spermatocidal agents and/orcontraceptive agents which aim to suppress fertility of spermatozoa,thrombolytic agents, conformation altering agents of saccharide-chains,agents for preventing arteriosclerosis, metabolism (lipids, sugar)improving agents, agents for wound healing, epithelialization promotingagents (including hair restoration effect), inhibitors and/or blockingagents which can control generation of function with bioactivesubstances (for example, enzymes, peptides, gene). In addition, thecompounds, the derivatives or those acid addition salt compounds caninhibit and/or block function generated by multi-dimensional structure(conformation) of the substance which consist of a shape and function ofliving organism. Moreover, the compounds, the derivatives or those acidaddition salt compounds provide chemical substances which can control,inhibit and/or block the function which is generated bymulti-dimensional structure (conformation) with macromoleculessubstances and macromolecules composite materials as well as livingorganism. In addition, when halogen compounds such as halogenated alkalimetals or halogenated alkali-earthy metals or halogenated zinc is addedin the compounds which were provided by this invention, a reaction isable to be induced. Moreover, when gold colloid is added in thecompounds which were provided by this invention, marking and/or labelingsubstances can be made and, it is also possible to use the compoundswhich were provided by this invention as dispersion (diffusion)preventives of tinction and printing dye, ink stabilizers or dyesticking agents. In addition, by using a color coupler such as dye withthe compounds which were provided by this invention, coloring of the dyecan be enhanced. When fragrant agents is used with the compounds whichwere provided in this invention, possible fragrance can be produced. Inaddition, the compounds, the derivatives or those acid addition saltcompounds can be utilized as depolymerization agents, surface-activeagents and/or surfactants, improving agents for surface activesubstances, phase transition agents, improving agents of phasetransition, improving agents of microphase separation structure,plasticity and/or elasticity promoting agents, plasticity and/orelasticity improving agents (plasticizers), copolymerization agents,copolymerization improving agents, polymerization regulators, improvingagents of polymerization adjustment, stabilizers, stabilizationimproving agents, antioxidants, oxidation preventing agents, improvingagents of rystailized materials and/or amorphous materials, fluidabilityimproving agents, flexibility promoters, improving agents for changingflexibility, improving agents of fluorescent wavelength and excitationwavelength of pigmentums, coating materials, cosmetic pigments andcolorants, alterable agents of fluorescent wavelength and excitationwavelength of pigmentums, coating materials, cosmetic pigments andcolorants. And, it is also possible to utilize the compounds, thederivatives or those acid addition salt compounds as the followingimproving agents. Those are agents which can improve physical propertyof low molecule substances, agents which can improve function of lowmolecule substances, agents which can improve physical property ofmacromolecules substance, agents which can improve function ofmacromolecules substances, agents which can improve physical property ofmacromolecules composite materials and functional macromoleculescomposite materials.

[0041] wherein

[0042] (i) R3, R4,. R5 and R6 represent independently hydrogen atom;halogen atom; C1-C6 alkyl group; amidino group; C3-C8 cycloalkyl group;C1-C6 alkoxy C1-C6 alkyl group; aryl group; allyl group; aralkyl groupin which one or more C1-C6 alkyl groups are bound to an aromatic ringselected from the group consisting of benzene, naphthalene andanthracene ring; C1-C6 alkylene group; benzoyl group; cinnamyl group;cinnamoyl group or furoyl group;

[0043] (ii) one or more of R3 and R4, and/or one or more of R5 and R6may be substituted or non-substituted cyclopentyl group; substituted ornon-substituted cyclohexyl group; or substituted or non-substitutednaphthyl group;

[0044] (iii) R5 and R6 may form a ring by binding with anothercondensation polycyclic hydrocarbon compound or heterocyclic compound;

[0045] (iv) one or more of R3, R4, R5 and R6 may be substituted by oneor more of substituents selected from the group consisting of halogenatom, cyano group, protected or non-protected carboxyl group, protectedor non-protected hydroxyl group, protected or non-protected amino group,C1-C6 alkyl group, C1-C6 alkoxy group, C1-C7 alkoxy carbonyl group, arylgroup, C3-C6 cycloalkyl group, C1-C6 acylamino group, C1-C6 acyloxygroup, C2-C6 alkenyl group, C1-C6 trihalogenoalkyl group, C1-C6alkylamino group, and C1-C6 dialkylamino group;

[0046] (v) R5 may be substituted by one or more substituents selectedfrom the group consisting of halogen atom, C1-C6 alkyl group, protectedor non-protected carboxyl group, protected or non-protected hydroxylgroup, protected or non-protected amino group, protected ornon-protected C1-C6 alkylamino group, protected or non-protected C1-C6aminoalkyl group, protected or non-protected C1-C6 alkylamino C1-C6alkyl group, protected or non-protected hydroxyalkyl group, and C3-C6cycloalkylamino group;

[0047] (vi) when one or more of R3, R4, R5 and R6 are alkyl groups,terminal end(s) of the alkyl group(s) may be substituted by C3-C8cycloalkyl group).

[0048] The aryl group in (i) and (iv) may be phenyl, tollyl, xylyl ornaphthyl group. The substituted cyclopentyl group in (ii) may becyclopentylamino group or cyclopentylcarbinol group, the substitutedcyclohexyl group in (ii) may be cyclohexylamino group,cyclohexylaldehyde group or cyclohexyl acetic acid group, and thesubstituted naphthyl group in (ii) may be naphthylamino group ornaphthylamino sulfonic acid-group. The condensation polycyclichydrocarbon compound in (iii) may be pentalene, indene, naphthalene,azulene, heptalene, biphenylene, indacene, acenaphthylene, fluorene,phenalene, phenanthrene, anthracene, pentacene, hexacene,dibenzophenanthrene, 1H-cyclopentacyclooctene or benzocyclooctene, andthe heterocyclic compound may be furan, thiophene, pyrrole, α-pyran,α-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole orquinoline.

[0049] The invention mentioned on claims 12-20 provides antibacterialagents, antifungal agents, antiviral agents, bactericidal and/orsterilized agents, anticancer drugs, anticoagulants and/orantifibrinolytic agents, blood coagulation and/or fibrinolysis blockingagents, inhibitory agents of antigen-antibody reaction, preservativesfor tissues and/or organs, and antiseptics and preservatives byutilizing effects on change in conformation, thermodynamic effect, phasetransition effect, flexibility changing effect, depolymerization effect,improving effect of macromolecules property, chemical kinetic effect,reduction effect, effect as free radical scavengers, desulfurizationeffect, antioxidant effect, nucleophilic and electrophilic effectsaccording to orbital dynamics of molecules and/or hydrophobic effect,which are inhibitory or blocking agents of molecular generating and/orinducing functions in claims 1-11.

[0050] The invention mentioned on claims 21 provides labeled regentswhich can detect a targeted position of generating function of molecule,utilizing effect on specific regions due to inhibitory or blockingagents of molecular generating and/or inducing functions in claims 1-11,and having a labeled substance at least in one substituent.

[0051] The invention mentioned on claims 22, 23 and 24 providesreductants, free radical scavengers and desufude agents utilizinginhibitory or blocking agents of molecular generating and/or inducingfunctions in claims 1-11.

[0052] The invention mentioned on claims 25-46 provides depolymerizationagents, improving agents for surface active substances, spermatocidalagents and/or contraceptive agents for external use, thrombolyticagents, conformation altering agents of saccharide-chains, agents forpreventing arteriosclerosis, metabolism (lipids, sugar) improvingagents, agents for wound healing, epithelialization promoting agents,phase transition agents, improving agents of phase transition, improvingagents of microphase separation structure, plasticity and/or elasticitypromoting agents, plasticity and/or elasticity improving agents(plasticizers), copolymerization agents, copolymerization improvingagents, polymerization regulators, improving agents of polymerizationadjustment, stabilizers, stabilization improving agents, antioxidants,oxidation preventing agents, improving agents of crystallized materialsand/or amorphous materials, fluidability improving agents, flexibilitypromoters (softers), improving agents for changing flexibility (softnerimproving agents), improving agents of excitation wavelength andfluorescent wavelength of colorants, pigmentums, coating materials andcosmetic pigments, and alterable agents of excitation wavelength andfluorescent wavelength of pigmentums, coating materials and cosmeticpigments, agents which can improve physical property of low moleculesubstances, agents which can improve function of low moleculesubstances, agents which can improve physical property of macromoleculessubstance, agents which can improve function of macromoleculessubstances, agents which can improve physical property of macromoleculescomposite materials and functional macromolecules composite materials.

[0053] In the present specification, unless otherwise specified, theterm “halogen atom” means, for example, fluorine atom, chlorine atom,bromine atom or iodine atom; the term “alkyl group” means C1-10 alkylgroup such as methyl group, ethyl group, n-propyl group, isopropylgroup, n-butyl group, isobutyl group, sec-butyl group, tort-butyl group,benzyl group, hexyl group, octyl group or the like; the term“lower-alkyl group” means C1-5 alkyl group among the alkyl groupsmentioned above; the term “alkoxy group” means —O— alkyl group (alkylgroup is C1-10 alkyl group mentioned above); the term “lower alkylaminogroup” means C1-5 alkylamino group such as methylamino group, ethylaminogroup, propylamino group or the like; the term “di-lower alkylaminogroup” means C1-5 dialkylamino group such as dimethylamino group; theterm “lower alkenyl group” means C2-5 alkenyl group such as vinyl group,allyl group, 1-propenyl group, 1-butenyl group or the like; the term“cycloalkyl group” means C3-6 cycloalkyl group such as cyclopropyl,cyclobutyl, cyclopentyl, cydlohexyl or the like; the term “aryl group”means, for example, phenyl group or naphthyl group; the term “alkoxycarbonyl group” means

[0054] —COO-alkyl group (alkyl group means C1-10 alkyl group abovementioned); the term “hydroxy lower alkyl group” means hydroxy-C1-5alkyl group such as hydroxy methyl group, hydroxy ethyl group, hydroxypropyl group or the like; the term “amino lower alkyl group” means aminoC1-5 alkyl group such as aminomethyl group, aminoethyl group,aminopropyl group or the like; the term “lower alkylamino lower alkylgroup” means C1-5 alkylamino C1-5 alkyl group such as methylaminomethylgroup, ethylaminomethyl group, ethylaminoethyl group or the like; theterm “di-lower alkylamino lower alkyl group” means C1-5 dialkylaminoC1-5 alkyl group such as dimethylaminomethyl group or diethylaminomethylgroup; the term “cyclic amino group” means cyclic amino group with 4-10membered ring such as piperazinyl group, morpholinyl group,1,4-diazabicyclo (3,2,1) octyl group or the like; the term “cyclic aminolower alkyl group” means C1-5 alkyl group attached to cyclic amino groupwith 4-6 membered ring such as 1-piperazinylmethyl group,1-pyrrolidinylmethyl group, 1-azethydinylmethyl group,1-morpholinylmethyl group or the like; the term “acylamino group” meansC1-4 acylamino group such as formylamino group, acetylamino group,propionylamino group, butyrylamino group or the like; the term “acyloxygroup” means C1-4 acyloxy group such as formyloxy group, acetyloxygroup, propionyloxy group, butyryloxy group or the like; the term“trihalogeno-lower alkyl group” means trihalogeno C1-5 alkyl group suchas trichloromethyl group, trifluoromethyl group or the like; the term“heterocyclic group” means 5 membered ring, 6 membered ring or thosecondensation rings (such as furyl, propyl, thienyl, oxazolyl,imidazolyl, thiazolyl, 1-pyrrolinyl, benzofuryl, benzothiazolyl,pyridyl, quinolyl, pyrimidinyl or morpholinyl group as an example) whichhas one or more atoms selected from the group consisting of oxygen atom,nitrogen atom and sulfate atom.

[0055] The alkyl group represented by R3, R4, R5, R6, R10 or R11 in eachgeneral formula may be either straight or branched alkyl group such as,for example, methyl group, ethyl group, propyl group, isopropyl group,butyl isobutyl group, sec-butyl group, 1-butyl group, pentyl group,isopentyl group, neopentyl group or hexyl group which are lower alkylgroups (C1-4). In addition, terminal end of these alkyl groups can bebound to lower cycloalkyl group (C3-4) such as cyclopropyl methyl group,cyclobutyl ethyl group, cyclopentyl methyl group or the like.

[0056] Lower cycloalkyl groups (C3-4) included in the cycloalkyl grouprepresented by R3, R4, R5, R6, R10 and R11 in each general formula maybe, for example, cyclopropyl group, cyclobutyl group, cyclopentyl groupor cyclohexyl group. The alkoxyalkyl group may be, for example, ethylgroup, methyl group, methoxyethyl group, ethoxyethyl group, propoxyethylgroup, isopropoxyethyl group, butoxyethyl group, methoxypropyl group,2-ethoxy-l-methyl ethyl group or the like.

[0057] Straight or branched alkylene group represented by R3, R4, R5,R6, R10 or R11 in each general formula may be, for example, methylenegroup, ethylene group, trimethylene group, tetramethylene group,1,2-dimethylethylene group or the like.

[0058] Each substituent of R3, R4, R5, R6, R10 and R11 in each generalformula or the methylene group in the general formula 3-a may be atleast one substituent selected from the group consisting of halogenatom, cyano group, protected or non-protected carboxyl group, protectedor non-protected hydroxyl group, protected or non-protected amino group,alkyl group, alkoxy group, alkoxy carbonyl group, aryl group, cycloalkylgroup, acylamino group, acyloxy group, lower alkenyl group,trihalogeno-lower alkyl group, lower alkylamino group, di-loweralkylamino group and the like; R2 and/or R5 may be substituted by atleast one substituent selected from the group consisting of halogenatom, lower alkyl group, protected or non-protected carboxyl group,protected or non-protected hydroxyl group, protected or non-protectedamino group, protected or non-protected lower alkylamino group,protected or non-protected amino lower alkyl group, protected ornon-protected lower alkylamino lower alkyl group, protected ornon-protected hydroxy lower alkyl group, di-lower alkylamino group,di-lower alkylamino lower alkyl group or cyclic amino lower alkyl group.

[0059] Examples of the protecting substituents of carboxyl group includepharmaceutically acceptable protecting groups of carboxyl group, such asan ester-forming group which is easily detached in an organism.

[0060] Moreover, protecting substituent of amino group, amino loweralkyl group, lower alkylamino group, and lower alkylamino lower alkylgroup may be a pharmaceutically acceptable amino-protecting group whichis easily detached in an organism.

[0061] In addition, protecting substituent of hydroxyl group and hydroxylower alkyl group may be a pharmaceutically acceptable protecting groupof hydroxyl group which is easily detached in an organism.

[0062] Though halogen compounds can be added to the compositionsaccording to this invention, it is necessary to give heed to anexistence of toxicity which the combined compounds may have. By addinghalogen compounds, coloring due to light can be prevented. Halogencompounds which can be applied to the compositions according to thisinvention, for example, are halogenated alkali metals such as potassiumbromide, sodium bromide, potassium chloride, sodium chloride, potassiumiodide and sodium iodide, and halogenated alkaline-earth metal such ascalcium bromide, magnesium bromide, calcium chloride and magnesiumchloride, and halogenated zinc such as zinc bromide and zinc chloride.

[0063] In addition, in the present specification, unless otherwisespecified, or except for the case which is clear from a context, theterm “alkyl group” includes straight alkyl group as well as branchedone. Similarly, the alkyl group in “alkoxy group”, “aralkyl group” and“alkylamino group” which has alkyl group includes straight alkyl groupas well as branched one. “Cycloalkyl group” is also similar to theabove, and includes branched groups such as ethyl cyclopentyl group andmethyl cyclohexyl group.

[0064] The compounds provided in this invention can be directly appliedon the surface of infected wound such as burn and decubitus. And, thosecan be used by combining with the carrier substances which are allowableon pharmaceutic use. In addition, when it is applied to living space,environment and at industry, those can be used during and/or aftermanufacturing step of materials according to the objective. Though it isnot restricted to representative applications, it is also possible to beadded those compounds on any manufacturing steps of surface processingby attaching, painting or spraying as agents to prevent bacterial andfungal proliferation and/or infection for construction materials,furnitures, lavatory goods, bathtub supplies, washing supplies, householding electric instruments and/or daily use goods. Moreover, whenthose compounds are utilized in a thread kneading and/or laterprocessing concerning any step of manufacturing fibers and thesematerials, effect of preventing bacterial and fungal proliferationand/or infection and an anti-allergic effect can be gained. An effect ofthe objective which is shown by claims can be made by using seats andfilm materials.

[0065] The carrier substances which is allowable on pharmaceutic use aregiven the carrier substances which is allowable biologically, such aspolyoxyalkylenealkyl ether, polyoxyethylene sorbitan fatty acid ester,polyvinylpyrrolidone, hydrocarbon, paraffin, alcohol, polyvalentalcohol, alcohol ester, polyalcohol ester, fatty acid and metal salts offatty acid. Moreover, chitosan, polyethylene glycol, polyethyleneglycerin fatty acid ester (caprylic acid, capric acid, lauric acid) canbe exemplified.

[0066] In addition, when the compounds mentioned in this invention areused as combined substances with the carrier substances which areallowable on pharmaceutic use, these can be applied in many kinds of thegenerally known agent types such as cream agents, ointments, pastes,poultices, milky lotions, suspensions, liniments, lotions, aerosolagents, solutions and tapes corresponding to prospected treatments.Also, it is allowed to add solvent supporting agents, isotonic changingagents, pH adjusters, deodorants, antiseptics or odorants in thecompounds mentioned in this invention. It is also possible to be addedthose compounds on any manufacturing steps of surface processing byattaching, painting or spraying as agents to prevent bacterial andfungal proliferation and/or infection for construction materials,furnitures, lavatory goods, bathtub supplies, washing supplies, householding electric instruments and/or daily use goods. Moreover, whenthose compounds are utilized in the thread kneading and/or laterprocessing concerning any step of manufacturing fibers and thesematerials, effect of preventing bacterial and fungal proliferationand/or infection and an anti-allergic effect can be gained. An effect ofthe objective can be made as wall papers and filters by using seat andfilm material. When it is used as spermatocidal agents and contraceptiveagents for external use, it is also possible to process surface ofcontraceptive possession such as condoms as well as ointments andcreams.

[0067] Below, details of this invention are explained. Inhibitory orblocking agents of functions generated by multi-dimensional structurewhich are used by this invention can be completed above-mentionedobjectives by use of the compounds alone, and can be utilized togetherwith acid addition salts, emulsifiers, ester agents or polymerizationagents, unless electric charge distribution and electric charge densityof molecule are changed drastically. It can be used in the followingform as an example; acid addition salts of the compounds which areprovided in chemical formula (1-a), (1-b), (2), (3-a) and (3-b)mentioned above are non-toxic salts which are allowable pharmaceuticallyand, those are inorganic acids such as hydrochloric acid, hydrobromicacid, phosphoric acid or sulfuric acid and organic acids such as aceticacid, citric acid, tartaric acid, lactic acid, succinic acid, fumaricacid, maleic acid or methasulfonic acid.

[0068] Concerning chemical formula (1-a) of this invention, thefollowing compounds in chemical formula (1-a) can be given asrepresentatives. But, it is not restricted this invention by thedefinitive representatives. Concretely, as alkanes which all of R1, R2,R3, R4, R5, R6, R8 and R9 are hydrogen atom and R7 is non-cyclichydrocarbon, for example, the following compounds are represented.

[0069] (1) 4-isopropyl-2-cyclohexen-1-one

[0070] (2) 4-isobutyl-2-cyclohexen-1-one

[0071] (3) 4-isopentyl-2-cyclohexen-1-one

[0072] (4) 4-isohexyl-2-cyclohexen-1-one and so on.

[0073] Moreover, as amine-hydrazines which all of R1, R2, R3, R4, R5,R6, R8 and R9 are hydrogen atom and R7 is nitrogen atom, for example,

[0074] (5) 4-dimethylamino-2-cyclohexen-1-one

[0075] (6) 4-dimethylhydrazono-2-cyclohexen-1-one

[0076] (7) 4-isopropylidenehydrazino-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0077] As phosphines and those analogs which all of R1, R2, R3, R4, R5,R6, R8 and R9 are hydrogen atom and R7 is phosphorus, arsenic orantimony, for example,

[0078] (8) 4-dimethylphosphinetolyl-2-cyclohexen-1-one

[0079] (9) 4-dimethylallylidenetolyl-2-cyclohexen-1-one

[0080] (10) 4-dimethylstibinetolyl-2-cyclohexen-1-one

[0081] (11) 4-dimethylbismuthinetriyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0082] As sulfide compounds which all of R1, R2, R3, R4, R5, R6, R8 andR9 are hydrogen atom and R7 is sulfate, for example,

[0083] (12) 4-isopropanesulfo-2-cyclohexen-1-one

[0084] (13) 4-isopropanesulfino-2-cyclohexen-1-one

[0085] (14) 4-isopropanesulfeno-2-cyclohexen-1-one and so on, and thoseacid addition salts are exemplified.

[0086] Concerning chemical formula (1-b) of this invention, thefollowing compounds in chemical formula (1-b) can be given asrepresentatives. But, it is not restricted this invention by thedefinitive representatives. Concretely, as alkanes which all of R1, R2,R3, R4, R5, R6, R8, R9, R10 and R11 are hydrogen atom and R7 isnon-cyclic hydrocarbon, for example, the following compounds arerepresented.

[0087] (1) 4-isopropyl-cyclohexane-1-one

[0088] (2) 4-isobutyl-cyclohexane-1-one

[0089] (3) 4-isopentyl-cyclohexane-1-one

[0090] (4) 4-isohexyl-cyclohexane-1-one and so on.

[0091] As amine-hydrazines which all of R1, R2, R3, R4, R5, R6, R8, R9,R10 and R11 are hydrogen atom and R7 is nitrogen atom, for example, thefollowing compounds are represented.

[0092] (5) 4-dimethylamino-cyclohexane-1-one

[0093] (6) 4-dimethylhydrazono-cyclohexane-1-one

[0094] (7) 4-isopropylidenehydrazino-cyclohexane-1-one and so on.

[0095] As phosphines and analogs which all of R1, R2, R3, R4, R5, R6,R8, R9, R10 and R11 are hydrogen atom and R7 is phosphorus, arsenic orantimony, for example, the following compounds are represented.

[0096] (8) 4-dimethylphosphinetriyl-cyclohexane-1-one

[0097] (9) 4-dimethylarsinetriyl-cyclohexane-1-one

[0098] (10) 4-dimethylstibinetriyl-cyclohexane-1-one

[0099] (11) 4-dimethylbismuthinetriyl-cyclohexane-1-one and so on.

[0100] As sulfide compounds which all of R1, R2, R3, R4, R5, R6, R8, R9,R10 and R11 are hydrogen atom and R7 is sulfate, for example,

[0101] (12) 4-isopropanesulfo-cyclohexane-1-one

[0102] (13) 4-isopropanesulfino-cyclohexane-1-one

[0103] (14) 4-isopropanesulfeno-cyclohexane-1-one and so on, and thoseacid addition salts are exemplified.

[0104] Concerning chemical formula (2) of this invention, the followingcompounds in chemical formula (2) can be given as representatives. But,it is not restricted this invention by the definitive representatives.Concretely, as alkanes which all of R3, R4, R5 and R6 are hydrogen atomand R1 and/or R2 are alkyl groups of non-cyclic saturated hydrocarbon,for example,

[0105] (15) 4,4,6-trimethyl-2-cyclohexen-1-one

[0106] (16) 4,4-dimethyl-6-ethyl-2-cyclohexen-1-one

[0107] (17) 4,4-dimethyl-6-propyl-2-cyclohexen-1-one

[0108] (18). 4,4-dimethyl-6-is opropyl-2-cyclohexen-1-one

[0109] (19) 6-butyl-4,4-dimethyl-2-cyclohexen-1-one

[0110] (20) 4,4-dimethyl-6-isobutyl-2-cyclohexen-1-one

[0111] (21) 6-benzyl-4,4-dimethyl-2-cyclohexen-1-one

[0112] (22) 4,4-dimethyl-6-hexyl-2-cyclohexen-1-one

[0113] (23) 4,4-dimethyl-6-octyl-2-cyclohexen-1-one and so on, and thoseacid addition salts are exemplified.

[0114] Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1and/or R2 are alkoxy groups of heterocyclic compounds, for example,

[0115] (24) 6-pentyloxy-4,4-dimethyl-2-cyclohexen-1-one

[0116] (25) 4,4-dimethyl-6-hexyloxy-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified. When all of R3, R4, R5, R6are hydrogen atoms and R1 and/or R2 are lower alkylamino group ofamines, for example,

[0117] (26) 4,4-dimethyl-6-methylamino-2-cyclohexen-1-one

[0118] (27) 4,4-dimethyl-6-ethylamino-2-cyclohexen-1-one

[0119] (28) 4,4-dimethyl-6-propylamino-2-cyclohexen-1-one

[0120] (29) 4,4-dimethyl-6-dimethylamino-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0121] Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1and/or R2 are alkenyl groups of non-cyclic unsaturation hydrocarbon, forexample,

[0122] (30) 6-vinyl-4,4-dimethyl-2-cyclohexen-1-one

[0123] (31) 6-allyl-4,4-dimethyl-2-cyclohexen-1-one

[0124] (32) 4,4-dimethyl-6-isopropenyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0125] Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1and/or R2 are cycloalkyl group of monocyclic hydrocarbon, for example,

[0126] (32) 6-cyclopropyl-4,4-dimethyl-2-cyclohexen-1-one

[0127] (32) 6-cyclobutyl-4,4-dimethyl-2-cyclohexen-1-one

[0128] (32) 6-cyclopentyl-4,4-dimethyl-2-cyclohexen-1-one

[0129] (32) 6-cyclohexyl-4,4-dimethyl-2-cyclohexen-1-one and so on, andthose acid additions are exemplified.

[0130] Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1and/or R2 are allyl group of aromatic hydrocarbon 1 valence group, forexample,

[0131] (32) 4,4-dimethyl-6-phenyl-2-cyclohexen-1-one

[0132] (32) 4,4-dimethyl-6-naphthyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0133] All of R3, R4, R5 and R6 may be hydrogen atoms and R1 and/or R2may be alkoxy carbonyl groups as ester. In addition, when all of R3, R4,R5 and R6 are hydrogen atoms and R1 and/or R2 are hydroxy lower alkylgroup, for example,

[0134] (33) 4,4-dimethyl-6-hydroxymethyl-2-cyclohexen-1-one

[0135] (34) 4,4-dimethyl-6-hydroxyethyl-2-cyclohexen-1-one

[0136] (35) 4,4-dimethyl-6-hydroxypropyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0137] Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1and/or R2 are amino lower alkyl group, for example,

[0138] (36) 6-aminomethyl-4,4-dimethyl-2-cyclohexen-1-one

[0139] (37) 6-aminoethyl-4,4-dimethyl-2-cyclohexen-1-one

[0140] (38) 6-aminopropyl-4,4-dimethyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0141] Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1and/or R2 are lower alkylamino lower alkyl group, for example,

[0142] (39) 4,4-dimethyl-6-methylaminomethyl-2-cyclohexen-1-one

[0143] (40) 4,4-dimethyl-6-ethylaminomethyl-2-cyclohexen-1-one

[0144] (41) 4,4-dimethyl-6-ethylaminoethyl-2-cyclohexen-1-one so on, andthose acid addition salts are exemplified.

[0145] Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1and/or R2 are di-lower alkylamino lower alkyl group, for example,

[0146] (42) 4,4-dimethyl-6-dimethylaminomethyl-2-cyclohexen-1-one

[0147] (43) 4,4-dimethyl-6-diethylaminomethyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0148] Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1and/or R2 are cyclic amino groups, for example,

[0149] (44) 4,4-dimethyl-6-piperazinyl-2-cyclohexen-1-one

[0150] (45) 4,4-dimethyl-6-morpholinyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0151] Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1and/or R2 are cyclic amino lower alkyl group, for example,

[0152] (46) 4,4-dimethyl-6-piperazinylethyl-2-cyclohexen-1-one

[0153] (47) 4,4-dimethyl-6-pyrrolinylmethyl-2-cyclohexen-1-one

[0154] (48) 6-azethydinylmethyl-4,4-dimethyl-2-cyclohexen-1-one

[0155] (49) 4,4-dimethyl-6-morpholinylmethyl-2-cyclohexen-1-one, and soon, and those acid addition salts are exemplified.

[0156] Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1and/or R2 are acylamiho group of monoacylamin group, for example,

[0157] (50) 4,4-dimethyl-6-formylamino-2-cyclohexen-1-one

[0158] (51) 6-acetylamino-4,4-dimethyl-2-cyclohexen-1-one

[0159] (52) 4,4-dimethyl-6-propionylamino-2-cyclohexen-1-one

[0160] (53) 6-butyrylamino-4,4-dimethyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0161] Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1and/or R2 are acyloxy group of ester, for example,

[0162] (54) 4,4-dimethyl-6-formyloxy-2-cyclohexen-1-one

[0163] (55) 6-acetyloxy-4,4-dimethyl-2-cyclohexen-1-one

[0164] (56) 4,4-dimethyl-6-propionyloxy-2-cyclohexen-1-one

[0165] (57) 6-butyryloxy-4,4-dimethyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0166] Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1and/or R2 are trihalogeno lower alkyl group, for example,

[0167] (58) 4,4-dimethyl-6-trichloromethyl-2-cyclohexen-1-one

[0168] (59) 4,4-dimethyl-6-trifluoromethyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0169] Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1and/or R2 are polycyclic group, for example,

[0170] (60) 4,4-dimethyl-6-furyl-2-cyclohexen-1-one

[0171] (61) 4,4-dimethyl-6-propyl-2-cyclohexen-1-one

[0172] (62) 4,4-dimethyl-6-thienyl-2-cyclohexen-1-one

[0173] (63) 4,4-dimethyl-6-isoxazolyl-2-cyclohexen-1-one

[0174] (64) 4,4-dimethyl-6-imidazolyl-2-cyclohexen-1-one

[0175] (65) 4,4-dimethyl-6-thiazolyl-2-cyclohexen-1-one

[0176] (66) 4,4-dimethyl-6-pyrrolinyl-2-cyclohexen-1-one

[0177] (67) 6-benzofuryl-4,4-dimethyl-2-cyclohexen-1-one

[0178] (68) 6-benzothiazolyl-4,4-dimethyl-2-cyclohexen-1-one

[0179] (69) 6-pyridyl-4,4-dimethyl-2-cyclohexen-1-one

[0180] (70) 4,4-dimethyl-6-quinolyl-2-cyclohexen-1-one

[0181] (71) 4,4-dimethyl-6-pyrimidinyl-2-cycloheken-1-one

[0182] (72) 4,4-dimethyl-6-morpholinyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0183] Concerning this invention, in the compounds provided by chemicalformula (3-a), the compound which all of substituent R3, R4, R5 are R6in chemical formula (3-a) are hydrogen atoms represents4,4-dimethyl-6-methylene-2-cyclohexen-1-,one, which is termed asYoshixol. And, as other representatives, the following compounds can begiven as representatives.

[0184] But, it is not restricted this invention by the definitiverepresentatives. Concretely, for example, when all of substituent R3and/or R4 are alkyl group of non-cyclic saturated hydrocarbon,

[0185] (73) 6-methylene-4,4,5-trimethyl-2-cyclohexen-1-one

[0186] (74) 4,4-dimethyl-5-ethyl-6-methylene-2-cyclohexen-1-one

[0187] (75) 4,4-dimethyl-5-propyl-6-methylene-2-cyclohexen-1-one

[0188] (76) 4,4-dimethyl-5-isopropyl-6-methylene-2-cyclohexen-1-one

[0189] (77) 5-butyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0190] (78) 4,4-dimethyl-5-isobutyl-6-methylene-2-cyclohexen-1-one

[0191] (79) 5-benzyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0192] (80) 4,4-dimethyl-5-hexyl-6-methylene-2-cyclohexen-1-one

[0193] (81) 4,4-dimethyl-5-octyl-6-methylene-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0194] For example, when substituent R3 and/or R4 are alkoxy group ofheterocyclic compound,

[0195] (82) 5-pentyloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0196] (83) 4,4-dimethyl-5-hexyloxy-6-methylene-2-cyclohexen-1-one andso on, and those acid addition salts are exemplified.

[0197] For example, when substituent R3 and/or R4 are lower alkylaminogroup of amines,

[0198] (84) 4,4-dimethyl-5-methylamino-6-methylene-2-cyclohexen-1-one

[0199] (85) 4,4-dimethyl-5-ethylamino-6-methylene-2-cyclohexen-1-one

[0200] (86) 4,4-dimethyl-5-propylamino-6-methylene-2-cyclohexen-1-one

[0201] (87) 4,4-dimethyl-5-dimethylamino-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0202] For example, when substituent R3 and/or R4 are alkenyl group ofnon-cyclic unsaturation hydrocarbon,

[0203] (88) 5-vinyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0204] (89) 5-allyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0205] (90) 4,4-dimethyl-5-isopropenyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0206] For example, when substituent R3 and/or R4 are cycloalkyl groupof monocyclic hydrocarbon,

[0207] (91) 5-cyclopropyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0208] (92) 5-cyclobutyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0209] (93) 5-cyclopentyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0210] (94) 5-cyclohexyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one andso on, and those acid addition salts are exemplified.

[0211] For example, when substituent R3 and/or R4 are allyl group ofaromatic hydrocarbon 1 valence group,

[0212] (95) 4,4-dimethyl-5-phenyl-6-methylene-2-cyclohexen-1-one

[0213] (96) 4,4-dimethyl-5-naphthyl-6-methylene-2-cyclohexen-1-one andso on, and those acid addition salts are exemplified.

[0214] Substituent R3, R4 are sometimes alkoxy carbonyl group aromatichydrocarbon 1 valence group allyl group of ester.

[0215] (98) 4,4-dimethyl-5-hydroxy methyl-6-methylene-2-cyclohexen-1-one

[0216] (99) 4,4-dimethyl-5-hydroxy ethyl-6-methylene-2-cyclohexen-1-one

[0217] (100) 4,4-dimethyl-5-hydroxypropyl-6-methylene-2-cyclohexen-1-one and so on, and those acid additionsalts are exemplified.

[0218] For example, when substituent R3 and/or R4 are amino lower alkylgroup,

[0219] (101) 5-aminomethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0220] (102) 5-aminoethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0221] (103) 5-aminopropyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0222] For example, when substituent R3 and/or R4 are lower alkylaminolower alkyl group,

[0223] (104)4,4-dimethyl-5-methylaminomethyl-6-methylene-2-cyclohexen-1-one

[0224] (105)4,4-dimethyl-5-ethylaminomethyl-6-methylene-2-cyclohexen-1-one

[0225] (106)4,4-dimethyl-5-ethylaminoethyl-6-methylene-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0226] For example, when substituent R3 and/or R4 are di-loweralkylamino lower alkyl group,

[0227] (107)4,4-dimethyl-5-dimethylaminomethyl-6-methylene-2-cyclohexen-1-one

[0228] (108)4,4-dimethyl-5-diethylaminomethyl-6-methylene-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0229] For example, when substituent R3 and/or R4 are cyclic aminogroups,

[0230] (109) 4,4-dimethyl-5-piperazinyl-6-methylene-72-cyclohexen-1-one

[0231] (110) 4,4-dimethyl-5-morpholinyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0232] For example, when substituent R3 and/or R4 are cycloamino loweralkyl group,

[0233] (111) 4,4-dimethyl-5-piperazinylethyl-6-methylene-2-cyclohexen-1-one

[0234] (112) 4,4-dimethyl-5-pyrrolinylmethyl-6-methylene-2-cyclohexen-1-one

[0235] (113)5-azethydinylmethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0236] (114)4,4-dimethyl-5-morpholinylmethyl-6-methylene-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0237] For example, when substituent R3 and/or R4 are acylamino group ofmonoacylamin group;

[0238] (115) 4,4-dimethyl-5-formylamino-6-methylene-2-cyclohexen-1-one

[0239] (116) 5-acetylamino-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0240] (117)4,4-dimethyl-5-propionylamino-6-methylene-2-cyclohexen-1-one

[0241] (118) 5-butyrylamino-4,4-dimethyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0242] For example, when substituent R3 and/or R4 are acyloxy group ofester,

[0243] (119) 4,4-dimethyl-5-formyloxy-6-methylene-2-cyclohexen-1-one

[0244] (120) 5-acetyloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0245] (121) 4,4-dimethyl-5-propionyloxy-6-methylene-2-cyclohexen-1-one

[0246] (122) 5-butyryloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0247] For example, when substituent R3 and/or R4 are trihalogeno loweralkyl group,

[0248] (123)4,4-dimethyl-5-trichloromethyl-6-methylene-2-cyclohexen-1-one

[0249] (124)4,4-dimethyl-5-trifluoromethyl-6-methylene-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0250] For example, when substituent R3 and/or R4 are polycyclic group,

[0251] (125) 4,4-dimethyl-5-furyl-6-methylene-2-cyclohexen-1-one

[0252] (126) 4, 4-dimethyl-5-propyl-6-methylene-2-cyclohexen-1-one

[0253] (127) 4,4-dimethyl-5-thienyl-6-methylene-2-cyclohexen-1-one

[0254] (128) 4,4-dimethyl-5-isoxazolyl-6-methylene-2-cyclohexen-1-one

[0255] (129) 4,4-dimethyl-5-imidazolyl-6-methylene-2-cyclohexen-1-one

[0256] (130) 4,4-dimethyl-5-thiazolyl-6-methylene-2-cyclohexen-1-one

[0257] (131) 4,4-dimethyl-5-pyrrolinyl-6-methylene-2-cyclohexen-1-one

[0258] (132) 5-benzofuryl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0259] (133)5-benzothiazolyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0260] (134) 5-pyridyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0261] (135) 4,4-dimethyl-5-quinolyl-6-methylene-2-cyclohexen-1-one

[0262] (136) 4,4-dimethyl-5-pyrimidinyl-6-methylene-2-cyclohexen-1-one

[0263] (137) 4,4-dimethyl-5-morpholinyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0264] For example, when substituent R5 is alkyl group of non-cyclicsaturated hydrocarbon,

[0265] (138) 3,4,4-trimethyl-6-methylene-2-cyclohexen-1-one

[0266] (139) 4,4-dimethyl-3-ethyl-6-methylene-2-cyclohexen-1-one

[0267] (140) 4,4-dimethyl-6-methylene-3-propyl-2-cyclohexen-1-one

[0268] (141) 4,4-dimethyl-3-isopropyl-6-methylene-2-cyclohexen-1-one

[0269] (142) 3-butyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0270] (143) 4,4-dimethyl-3-isobutyl-6-methylene-2-cyclohexen-1-one

[0271] (144) 3-benzyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0272] (145) 4,4-dimethyl-3-hexyl-6-methylene-2-cyclohexen-1-one

[0273] (146) 4,4-dimethyl-6-methylene-3-octyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0274] For example, when substituent R5 is alkoxy group of heterocycliccompound,

[0275] (147) 3-pentyloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0276] (148) 4,4-dimethyl-3-hexyloxy-6-methylene-2-cyclohexen-1-one andso on, and those acid addition salts are exemplified.

[0277] For example, when substituent R5 is lower alkylamino group ofamine group,

[0278] (149) 4,4-dimethyl-3-methylamino-6-methylene-2-cyclohexen-1-one

[0279] (150) 4,4-dimethyl-3-ethylamino-6-methylene-2-cyclohexen-1-one(151) 4,4-dimethyl-6-methylene-3-propylamino-2-cyclohexen-1-one

[0280] (152) 4,4-dimethyl-3-dimethylamino-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0281] For example, when substituent R5 is alkenyl group of non-cyclicunsaturation hydrocarbon,

[0282] (153) 3-vinyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0283] (154) 3-allyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0284] (155) 4,4-dimethyl-3-isopropenyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0285] For example, when substituent R5 is cycloalkyl group ofmonocyclic hydrocarbon,

[0286] (156) 3-cyclopropyl-4, 4-dimethyl-6-methylene-2-cyclohexen-1-one

[0287] (157) 3-cyclobutyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0288] (158) 3-cyclopentyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0289] (159) 3-cyclohexyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0290] For example, when substituent R5 is allyl group of aromatichydrocarbon 1 valence group,

[0291] (160) 4,4-dimethyl-3-phenyl-6-methylene-2-cyclohexen-1-one

[0292] (161) 4,4-dimethyl-6-methylene-3-naphthyl-2-cyclohexen-1-one andso on, and those acid addition salts are exemplified. Substituent R5 isalkoxy carbonyl group and the compound becomes ester. For example, whensubstituent R5 is hydroxy lower alkyl group,

[0293] (163) 4,4-dimethyl-3-hydroxymethyl-6-methylene-2-cyclohexen-1-one

[0294] (164) 4,4-dimethyl-3-hydroxy ethyl-6-methylene-2-cyclohexen-1-one

[0295] (165) 4,4-dimethyl-3-hydroxypropyl-6-methylene-2-cyclohexen-1-one and so on, and those acid additionsalts are exemplified.

[0296] For example, when substituent R5 is an amino lower alkyl group,

[0297] (166) 3-aminomethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0298] (167) 3-aminoethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0299] (168) 3-aminopropyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0300] For example, when substituent R5 is a lower alkylamino loweralkyl group,

[0301] (169)4,4-dimethyl-3-methylaminomethyl-6-methylene-2-cyclohexen-1-one

[0302] (170)4,4-dimethyl-3-ethylaminomethyl-6-methylene-2-cyclohexen-1-one

[0303] (171)4,4-dimethyl-3-ethylaminoethyl-6-methylene-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0304] For example, when substituent R5 is a lower alkylamino loweralkyl group,

[0305] (172)3-dimethylaminomethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0306] (173)3-diethylaminomethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0307] For example, when substituent R5 is cyclic amino group,

[0308] (174) 4,4-dimethyl-6-methylene-3-piperazinyl-2-cyclohexen-1-one

[0309] (175) 4,4-dimethyl-6-methylene-3-morpholinyl-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0310] For example, when substituent R5 is cyclic amino lower alkylgroup,

[0311] (176) 4,4-dimethyl-6-methylene-3-piperazinylethyl-2-cyclohexen-1-one

[0312] (177) 4,4-dimethyl-6-methylene-3-pyrrolinylmethyl-2-cyclohexen-1-one

[0313] (178)3-azethydinylmethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0314] (179)4,4-dimethyl-6-methylene-3-morpholinylmethyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0315] For example, when substituent R5 is acylamino group ofmonoacylamin,

[0316] (180) 4,4-dimethyl-3-formylamino-6-methylene-2-cyclohexen-1-one

[0317] (181) 3-acetylamino-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0318] (182)4,4-dimethyl-6-methylene-3-propionylamino-2-cyclohexen-1-one

[0319] (183) 3-butyrylamino-4,4-dimethyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0320] For example, when substituent R5 is acyloxy group of ester,

[0321] (184) 4,4-dimethyl-3-formyloxy-6-methylene-2-cyclohexen-1-one

[0322] (185) 3-acetyloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0323] (186) 4,4-dimethyl-6-methylene-3-propionyloxy-2-cyclohexen-1-one

[0324] (187) 3-butyryloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0325] For example, when substituent R5 is a trihalogeno lower alkylgroup,

[0326] (188)4,4-dimethyl-6-methylene-3-trichloromethyl-2-cyclohexen-1-one

[0327] (189)4,4-dimethyl-6-methylene-3-trifluoromethyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0328] For example, when substituent R5 is polycyclic group,

[0329] (190) 4,4-dimethyl-3-furyl-6-methylene-2-cyclohexen-1-one

[0330] (191) 4,4-dimethyl-6-methylene-3-propyl-2-cyclohexen-1-one

[0331] (192) 4,4-dimethyl-6-methylene-3-thienyl-2-cyclohexen-1-one

[0332] (193) 4,4-dimethyl-3-isoxazolyl-6-methylene-2-cyclohexen-1-one

[0333] (194) 4,4-dimethyl-3-imidazolyl-6-methylene-2-cyclohexen-1-one

[0334] (195) 4,4-dimethyl-6-methylene-3-thiazolyl-2-cyclohexen-1-one

[0335] (196) 4,4-dimethyl-6-methylene-3-pyrrolinyl-2-cyclohexen-1-one

[0336] (197) 3-benzofuryl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0337] (198)3-benzothiazolyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0338] (199) 3-pyridyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0339] (200) 4,4-dimethyl-6-methylene-3-quinolyl-2-cyclohexen-1-one

[0340] (201) 4,4-dimethyl-6-methylene-3-pyrimidinyl-2-cyclohexen-1-one

[0341] (202) 4,4-dimethyl-6-methylene-3-morpholinyl-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0342] For example, when substituent R6 is alkyl group of non-cyclicsaturated hydrocarbon,

[0343] (203) 6-methylene-2,4,4-trimethyl-2-cyclohexen-1-one

[0344] (204) 4,4-dimethyl-2-ethyl-6-methylene-2-cyclohexen-1-one

[0345] (205) 4,4-dimethyl-6-methylene-2-propyl-2-cyclohexen-1-one

[0346] (206) 4,4-dimethyl-2-isopropyl-6-methylene-2-cyclohexen-1-one

[0347] (207) 2-butyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0348] (208) 4,4-dimethyl-2-isobutyl-6-methylene-2-cyclohexen-1-one

[0349] (209) 2-benzyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0350] (210) 4,4-dimethyl-2-hexyl-6-methylene-2-cyclohexen-1-one

[0351] (211) 4,4-dimethyl-6-methylene-2-octyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0352] For example, when substituent R6 is alkoxy group of heterocycliccompound,

[0353] (212) 2-pentyloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-one(213) 4,4-dimethyl-2-hexyloxy-6-methylene-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0354] For example, when substituent R6 is a lower alkylamino group ofamines,

[0355] (214) 4,4-dimethyl-2-methylamino-6-methylene-2-cyclohexen-1-one

[0356] (215) 4,4-dimethyl-2-ethylamino-6-methylene-2-cyclohexen-1-one

[0357] (216) 4,4-dimethyl-6-methylene-2-propylamino-2-cyclohexen-1-one

[0358] (2-17)2-dimethylamino-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0359] For example, when substituent R6 is alkenyl group of non-cyclicsaturated hydrocarbon,

[0360] (218) 2-vinyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0361] (219) 2-allyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0362] (220) 4,4-dimethyl-2-isopropenyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0363] For example, when substituent R6 is cycloalkyl group ofmonocyclic hydrocarbon,

[0364] (221) 2-cyclopropyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0365] (222) 2-cyclobutyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0366] (223) 2-cyclopentyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0367] (224) 2-cyclohexyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0368] For example, when substituent R6 is allyl group of aromatichydrocarbon 1 valence group,

[0369] (225) 4,4-dimethyl-2-phenyl-6-methylene-2-cyclohexen-1-one

[0370] (226) 4,4-dimethyl-6-methylene-2-naphthyl-2-cyclohexen-1-one andso on, and those acid addition salts are exemplified.

[0371] Substituent R6 is alkoxy carbonyl group resulting in ester.

[0372] For example, when substituent R6 is a hydroxy lower alkyl group,

[0373] (228) 4,4-dimethyl-2-hydroxymethyl-6-methylene-2-cyclohexen-1-one

[0374] (229) 4,4-dimethyl-2-hydroxy ethyl-6-methylene-2-cyclohexen-1-one

[0375] (230) 4,4-dimethyl-2-hydroxypropyl-6-methylene-2-cyclohexen-1-one and so on, and those acid additionsalts are exemplified.

[0376] For example, when substituent R6 is an amino lower alkyl group,

[0377] (231) 2-aminomethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0378] (232) 2-aminoethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0379] (233) 2-aminopropyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0380] For example, when substituent R6 is a lower alkylamino loweralkyl group,

[0381] (234)4,4-dimethyl-2-methylaminomethyl-6-methylene-2-cyclohexen-1-one

[0382] (235)4,4-dimethyl-2-ethylaminomethyl-6-methylene-2-cyclohexen-1-one

[0383] (236)4,4-dimethyl-2-ethylaminoethyl-6-methylene-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0384] For example, when substituent R6 is a di-lower alkylamino loweralkyl group,

[0385] (237)2-dimethylaminomethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0386] (238)2-diethylaminomethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0387] For example, when substituent R6 is cyclic amino group,

[0388] (239) 4,4-dimethyl-6-methylene-2-piperazinyl-2-cyclohexen-1-one

[0389] (240) 4,4-dimethyl-6-methylene-2-morpholinyl-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0390] For example, when substituent R6 is a cyclic amino lower alkylgroup,

[0391] (241) 4,4-dimethyl-6-methylene-2-piperazinylethyl-2-cyclohexen-1-one

[0392] (242) 4,4-dimethyl-6-methylene-2-pyrrolinylmethyl-2-cyclohexen-1-one

[0393] (243)2-azethydinylmethyl-4,4-dimethyl-6-methylene-,2-cyclohexen-1-one

[0394] (244)4,4-dimethyl-6-methylene-2-morpholinylmethyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0395] For example, when substituent R6 is acylamino group ofmonoacylamin,

[0396] (245) 4,4-dimethyl-2-formylamino-6-methylene-2-cyclohexen-1-one

[0397] (246) 2-acetylamino-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0398] (247)4,4-dimethyl-6-methylene-2-propionylamino-2-cyclohexen-1-one

[0399] (248) 2-butyrylamino-4,4-dimethyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0400] For example, when substituent R6 is acyloxy group of ester,

[0401] (249) 4,4-dimethyl-2-formyloxy-6-methylene-2-cyclohexen-1-one

[0402] (250) 2-acetyloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0403] (251) 4,4-dimethyl-6-methylene-2-propionyloxy-2-cyclohexen-1-one

[0404] (252) 2-butyryloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0405] For example, when substituent R6 is a trihalogeno lower alkylgroup,

[0406] (253)4,4-dimethyl-6-methylene-2-trichloromethyl-2-cyclohexen-1-one

[0407] (254)4,4-dimethyl-6-methylene-2-trifluoromethyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified. For example, whensubstituent R6 is polycyclic group,

[0408] (255) 4,4-dimethyl-2-furyl-6-methylene-2-cyclohexen-1-one

[0409] (256) 4,4-dimethyl-6-methylene-2-propyl-2-cyclohexen-1-one

[0410] (257) 4,4-dimethyl-6-methylene-2-thienyl-2-cyclohexen-1-one

[0411] (258) 4,4-dimethyl-2-isoxazolyl-6-methylene-2-cyclohexen-1-one

[0412] (259) 4,4-dimethyl-2-imidazolyl-6-methylene-2-cyclohexen-1-one

[0413] (260) 4,4-dimethyl-6-methylene-2-thiazolyl-2-cyclohexen-1-one

[0414] (261) 4,4-dimethyl-6-methylene-2-pyrrolinyl-2-cyclohexen-1-one

[0415] (262) 2-benzofuryl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0416] (263)2-benzothiazolyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0417] (264) 2-pyridyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one

[0418] (265) 4,4-dimethyl-6-methylene-2-quinolyl-2-cyclohexen-1-one

[0419] (267) 4,4-dimethyl-6-methylene-2-pyrimidinyl-2-cyclohexen-1-one

[0420] (268) 4,4-dimethyl-6-methylene-2-morpholinyl-2-cyclohexen-1-oneand so on, and those acid addition salts are exemplified.

[0421] For example, when R5 and/or R6 in chemical formula (3-a) are bondsubstituent such as condensation polycyclic hydrocarbons andheterocyclic compounds,

[0422] (269) 5H-4-dimethyl-6-methylene-7-oxo-indene

[0423] (270) 4-dimethyl-2-methylene-1-oxo-tetralin

[0424] (271) 3H-4-dimethyl-2-methylene-1-oxo-anthracene

[0425] (272) 5H-4-dimethyl-6-methylene-7-oxo-benzothiophene

[0426] (273) 5H-4-dimethyl-6-methylene-7-oxo-benzofuran

[0427] (274) 5H-4-dimethyl-6-methylene-7-oxo-indole

[0428] (275) 6H-5-dimethyl-7-methylene-8-oxo-quinoline

[0429] (276) 6H-5-dimethyl-7-methylene-8-oxo-quinoxaline

[0430] (277) 6H-5-dimethyl-7-methylene-8-oxo-cinnoline

[0431] (278) 5H-5-dimethyl-7-methylene-8-oxo-1,4 dithianaphthalene

[0432] (279) 3H-4-dimethyl-2-methylene-1-oxo-thianthrene and so on, andthose acid addition salts are exemplified.

[0433] Concerning this invention, in the compounds provided by chemicalformula (3-b), the compound which all of substituent R3, R4, R5 are R6in chemical formula (3-b) are hydrogen atoms represents4,4-dimethyl-2-cyclohexen-1-one. And, as other representatives, thefollowing compounds can be given as representatives. But, it is notrestricted-this invention by the definitive representatives.

[0434] Concretely, when all of substituent R3 and/or R4 are alkyl groupof non-cyclic saturated hydrocarbon,-

[0435] (280) 4,4,5-trimethyl-2-cyclohexen-1-one

[0436] (281) 4,4-dimethyl-5-ethyl-2-cyclohexen-1-one

[0437] (282) 4,4-dimethyl-5-propyl-2-cyclohexen-1-one

[0438] (283) 4,4-dimethyl-5-isopropyl-2-cyclohexen-1-one

[0439] (284) 5-butyl-4,4-dimethyl-2-cyclohexen-1-one

[0440] (285) 4,4-dimethyl-5-isobutyl-2-cyclohexen-1-one

[0441] (286) 5-benzyl-4,4-dimethyl-2-cyclohexen-1-one

[0442] (287) 4,4-dimethyl-5-hexyl-2-cyclohexen-1-one

[0443] (288) 4,4-dimethyl-5-octyl-2-cyclohexen-1-one and so on, and.those acid addition salts are exemplified.

[0444] For example, when substituent R3 and/or R4 are alkoxy groups ofheterocyclic compound,

[0445] (289) 5-pentyloxy-4,4-dimethyl-2-cyclohexen-1-one

[0446] (290) 4,4-dimethyl-5-hexyloxy-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified. For example, when substituentR3 and/or R4 are lower alkylamino group of amines,

[0447] (291) 4,4-dimethyl-5-methylamino-2-cyclohexen-1-one

[0448] (292) 4,4-dimethyl-5-ethylamino-2-cyclohexen-1-one

[0449] (293) 4,4-dimethyl-5-propylamino-2-cyclohexen-1-one

[0450] (294) 4,4-dimethyl-5-dimethylamino-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0451] For example, when substituent R3 and/or R4 are alkenyl group ofnon-cyclic unsaturation hydrocarbon,

[0452] (295) 5-vinyl-4,4-dimethyl-2-cyclohexen-1-one

[0453] (296) 5-allyl-4,4-dimethyl-2-cyclohexen-1-one

[0454] (297) 4,4-dimethyl-5-isopropenyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0455] For example, when substituent R3 and/or R4 are cycloalkyl groupof monocyclic hydrocarbon,

[0456] (298) 5-cyclopropyl-4,4-dimethyl-2-cyclohexen-1-one

[0457] (299) 5-cyclobutyl-4,4-dimethyl-2-cyclohexen-1-one

[0458] (300) 5-cyclopentyl-4,4-dimethyl-2-cyclohexen-1-one

[0459] (301) 5-cyclohexyl-4,4-dimethyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0460] For example, when substituent R3 and/or R4 are allyl group ofaromatic hydrocarbon 1 valence group,

[0461] (302) 4,4-dimethyl-5-phenyl-2-cyclohexen-1-one

[0462] (303) 4,4-dimethyl-5-naphthyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified. Substituent R3 and/or R4 aresometimes alkoxy carbonyl aromatic hydrocarbon 1 valence group and/orallyl group of ester.

[0463] (305) 4,4-dimethyl-5-hydroxy methyl-2-cyclohexen-1-one

[0464] (306) 4,4-dimethyl-5-hydroxy ethyl-2-cyclohexen-1-one

[0465] (307) 4,4-dimethyl-5-hydroxy propyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0466] For example, when substituent R3 and/or R4 are amino lower alkylgroup,

[0467] (308) 5-aminomethyl-4,4-dimethyl-2-cyclohexen-1-one

[0468] (309) 5-aminoethyl-4,4-dimethyl-2-cyclohexen-1-one

[0469] (310) 5-aminopropyl-4,4-dimethyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0470] For example, when substituent R3 and/or R4 are lower alkylaminolower alkyl group,

[0471] (311) 4,4-dimethyl-5-methylaminomethyl-2-cyclohexen-1-one

[0472] (312) 4,4-dimethyl-5-ethylaminomethyl-2-cyclohexen-1-one

[0473] (313) 4,4-dimethyl-5-ethylaminoethyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0474] For example, when substituent R3 and/or R4 are di-lower alkylamiolower alkyl group,

[0475] (314) 4,4-dimethyl-5-dimethylaminomethyl-2-cyclohexen-1-one

[0476] (315) 4,4-dimethyl-5-diethylaminomethyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0477] For example, when substituent R3 and/or R4 are cyclic aminogroups,

[0478] (316) 4,4-dimethyl-5-piperazinyl-2-cyclohexen-1-one

[0479] (317) 4,4-dimethyl-5-morpholinyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0480] For example, when substituent R3 and/or R4 are cyclic amino loweralkyl group,

[0481] (318) 4,4-dimethyl-5-piperazinyl ethyl-2-cyclohexen-1-one

[0482] (319) 4,4-dimethyl-5-pyrrolinyl methyl-2-cyclohexen-1-one

[0483] (320) 5-azethydinylmethyl-4,4-dimethyl-2-cyclohexen-1-one

[0484] (321) 4,4-dimethyl-5-morpholinylmethyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0485] For example, when substituent R3 and/or R4 are acylamino groupsof monoacylamin,

[0486] (322) 4,4-dimethyl-5-formylamino-2-cyclohexen-1-one

[0487] (323) 5-acetylamino-4,4-dimethyl-2-cyclohexen-1-one

[0488] (324) 4,4-dimethyl-5-propionylamino-2-cyclohexen-1-one

[0489] (325) 5-butyrylamino-4,4-dimethyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0490] For example, when substituent R3 and/or R4 are acyloxy group ofester,

[0491] (326) 4,4-dimethyl-5-formyloxy-2-cyclohexen-1-one

[0492] (327) 5-acetyloxy-4,4-dimethyl-2-cyclohexen-1-one

[0493] (328) 4,4-dimethyl-5-propionyloxy-2-cyclohexen-1-one

[0494] (329) 5-butyryloxy-4,4-dimethyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0495] For example, when substituent R3 and/or R4 are trihalogeno loweralkyl group,

[0496] (330) 4,4-dimethyl-5-trichloromethyl-2-cyclohexen-1-one

[0497] (331) 4,4-dimethyl-5-trifluoromethyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0498] For example, when substituent R3 and/or R4 are polycyclic groups,

[0499] (332) 4,4-dimethyl-5-furyl-2-cyclohexen-1-one

[0500] (333) 4,4-dimethyl-5-propyl-2-cyclohexen-1-one

[0501] (334) 4,4-dimethyl-5-thienyl-2-,cyclohexen-1-one

[0502] (335) 4,4-dimethyl-5-isoxazolyl-2-cyclohexen-1-one

[0503] (336) 4,4-dimethyl-5-imidazolyl-2-cyclohexen-1-one

[0504] (337) 4,4-dimethyl-5-thiazolyl-2-cyclohexen-1-one

[0505] (338) 4,4-dimethyl-5-pyrrolinyl-2-cyclohexen-1-one

[0506] (339) 5-benzofuryl-4,4-dimethyl-2-cyclohexen-1-one

[0507] (340) 5-benzothiazolyl-4,4-dimethyl-2-cyclohexen-1-one

[0508] (341) 5-pyridyl-4,4-dimethyl-2-cyclohexen-1-one

[0509] (342) 4,4-dimethyl-5-quinolyl-2-cyclohexen-1-one

[0510] (343) 4,4-dimethyl-5-pyrimidinyl-2-cyclohexen-1-one

[0511] (344) 4,4-dimethyl-5-morpholinyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0512] For example, when substituent R5 is alkyl group of non-cyclicsaturated hydrocarbon,

[0513] (345) 3,4,4-trimethyl-2-cyclohexen-1-one

[0514] (346) 4,4-dimethyl-3-ethyl-2-cyclohexen-1-one

[0515] (347) 4,4-dimethyl-3-propyl-2-cyclohexen-1-one

[0516] (348) 4,4-dimethyl-3-isopropyl-2-cyclohexen-1-one

[0517] (349) 3-butyl-4,4-dimethyl-2-cyclohexen-1-one

[0518] (350) 4,4-dimethyl-3-isobutyl-2-cyclohexen-1-one

[0519] (351) 3-benzyl-4,4-dimethyl-2-cyclohexen-1-one

[0520] (352) 4,4-dimethyl-3-hexyl-2-cyclohexen-1-one

[0521] (353) 4,4-dimethyl-3-octyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0522] For example, when substituent R5 is alkoxy group of heterocycliccompound,

[0523] (354) 3-pentyloxy-4,4-dimethyl-2-cyclohexen-1-one

[0524] (355) 4,4-dimethyl-3-hexyloxy-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified. For example, when substituentR5 is a lower alkylamino group of amines,

[0525] (356) 4,4-dimethyl-3-methylamino-2-cyclohexen-1-one

[0526] (357) 4,4-dimethyl-3-ethylamino-2-cyclohexen-1-one

[0527] (358) 4,4-dimethyl-3-propylamino-2-cyclohexen-1-one

[0528] (359) 3-dimethylamino-4,4-dimethyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0529] For example, when substituent R5 is alkenyl group of non-cyclicunsaturation hydrocarbon,

[0530] (360) 3-vinyl-4,4-dimethyl-2-cyclohexen-1-one

[0531] (361) 3-allyl-4,4-dimethyl-2-cyclohexen-1-one

[0532] (362) 4,4-dimethyl-3-isopropenyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0533] For example, when substituent R5 is cycloalkyl group ofmonocyclic hydrocarbon,

[0534] (363) 3-cyclopropyl-4,4-dimethyl-2-cyclohexen-1-one

[0535] (364) 3-cyclobutyl-4,4-dimethyl-2-cyclohexen-1-one

[0536] (365) 3-cyclopentyl-4,4-dimethyl-2-cyclohexen-1-one

[0537] (366) 3-cyclohexyl-4,4-dimethyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0538] For example, when substituent R5 is allyl group of aromatichydrocarbon 1 valence group,

[0539] (367) 4,4-dimethyl-3-phenyl-2-cyclohexen-1-one

[0540] (368) 4,4-dimethyl-3-naphthyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified. Substituent R5 is alkoxycarbonyl group resulting in ester.

[0541] For example, when substituent R5 is hydroxy lower alkyl group,

[0542] (370) 4,4-dimethyl -3-hydroxy methyl-2-cyclohexen-1-one

[0543] (371) 4,4-dimethyl -3-hydroxy ethyl-2-cyclohexen-1-one

[0544] (372) 4,4-dimethyl -3-hydroxy propyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0545] For example, when substituent R5 is amino lower alkyl group,

[0546] (373) 3-aminomethyl-4,4-dimethyl-2-cyclohexen-1-one

[0547] (374) 3-aminoethyl-4,4-dimethyl-2-cyclohexen-1-one

[0548] (375) 3-aminopropyl-4,4-dimethyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0549] For example, when substituent R5 is a lower alkylamino loweralkyl group,

[0550] (376) 4,4-dimethyl-3-methylaminomethyl-2-cyclohexen-1-one

[0551] (377) 4,4-dimethyl-3-ethylaminomethyl-2-cyclohexen-1-one

[0552] (378) 4,4-dimethyl-3-ethylaminoethyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0553] For example, when substituent R5 is a di-lower alkylamino loweralkyl group,

[0554] (379) 3-dimethylaminomethyl-4,4-dimethyl-2-cyclohexen-1-one

[0555] (380) 3-diethylaminomethyl-4,4-dimethyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0556] For example, when substituent R5 is cyclic amino group,

[0557] (381) 4,4-dimethyl-3-piperazinyl-2-cyclohexen-1-one

[0558] (382) 4,4-dimethyl-3-morpholinyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0559] For example, when substituent R5 is a cyclic amino lower alkylgroup,

[0560] (383) 4,4-dimethyl-3-piperazinylethyl-2-cyclohexen-1-one

[0561] (384) 4,4-dimethyl-3-pyrrolinylmethyl-2-cyclohexen-1-one

[0562] (385) 3-azethydinylmethyl-4,4-dimethyl-2-cyclohexen-1-one

[0563] (386) 4,4-dimethyl-3-morpholinylmethyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0564] For example, when substituent R5 is acylamino group ofmonoacylamin,

[0565] (387) 4,4-dimethyl-3-formylamin6-2-cyclohexen-1-one

[0566] (388) 3-acetylamino-4,4-dimethyl-2-cyclohexen-1-one

[0567] (389) 4,4-dimethyl-3-propionylamino-2-cyclohexen-1-one

[0568] (390) 3-butyrylamino-4,4-dimethyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0569] For example, when substituent R5 is acyloxy group of ester,

[0570] (391) 4,4-dimethyl-3-formyloxy-2-cyclohexen-1-one

[0571] (392) 3-acetyloxy-4,4-dimethyl-2-cyclohexen-1-one

[0572] (393) 4,4-dimethyl-3-propionyloxy-2-cyclohexen-1-one

[0573] (394) 3-butyryloxy-4,4-dimethyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0574] For example, when substituent R5-is a trihalogeno lower alkylgroup,

[0575] (395) 4,4-dimethyl-3-trichloromethyl-2-cyclohexen-1-one

[0576] (396) 4,4-dimethyl-3-trifluoromethyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0577] For example, when substituent R5 is polycyclic group,

[0578] (397) 4,4-dimethyl-3-furyl-2-cyclohexen-1-one

[0579] (398) 4,4-dimethyl-3-propyl-2-cyclohexen-1-one

[0580] (399) 4,4-dimethyl-3-thienyl-2-cyclohexen-1-one

[0581] (400) 4,4-dimethyl-3-isoxazolyl-2-cyclohexen-1-one

[0582] (401) 4,4-dimethyl-3-imidazolyl-2-cyclohexen-1-one

[0583] (402) 4,4-dimethyl-3-thiazolyl-2-cyclohexen-1-one

[0584] (403) 4,4-dimethyl-3-pyrrolinyl-2-cyclohexen-1-one

[0585] (404) 3-benzofuryl-4,4-dimethyl-2-cyclohexen-1-one

[0586] (405) 3-benzothiazolyl-4,4-dimethyl-2-cyclohexen-1-one

[0587] (406) 3-pyridyl-4,4-dimethyl-2-cyclohexen-1-one

[0588] (407) 4,4-dimethyl-3-quinolyl-2-cyclohexen-1-one

[0589] (408) 4,4-dimethyl-3-pyrimidinyl-2-cyclohexen-1-one

[0590] (409) 4,4-dimethyl-3-morpholinyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0591] For example, when substituent R6 is alkyl group of non-cyclicsaturated hydrocarbon,

[0592] (410) 2,4,4-trimethyl-2-cyclohexen-1-one

[0593] (411) 4,4-dimethyl-2-ethyl-2-cyclohexen-1-one

[0594] (412) 4,4-dimethyl-2-propyl-2-cyclohexen-1-one

[0595] (413) 4,4-dimethyl-2-isopropyl-2-cyclohexen-1-one

[0596] (414) 2-butyl-4,4-dimethyl-2-cyclohexen-1-one

[0597] (415) 4,4-dimethyl-2-isobutyl-2-cyclohexen-1-one

[0598] (416) 2-benzyl-4,4-dimethyl-2-cyclohexen-1-one

[0599] (417) 4,4-dimethyl-2-hexyl-2-cyclohexen-1-one

[0600] (418) 4,4-dimethyl-2-octyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0601] For example, when substituent R6 is alkoxy group of heterocycliccompound,

[0602] (419) 2-pentyloxy-4,4-dimethyl-2-cyclohexen-1-one

[0603] (420) 4,4-dimethyl-2-hexyloxy-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified. For example, when substituentR6 is a lower alkylamino group of amines,

[0604] (421) 4,4-dimethyl-2-methylamino-2-cyclohexen-1-one

[0605] (422) 4,4-dimethyl-2-ethylamino-2-cyclohexen-1-one

[0606] (423) 4,4-dimethyl-2-propylamino-2-cyclohexen-1-one

[0607] (424) 2-dimethylamino-4,4-dimethyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0608] For example, when substituent R6 is alkenyl group of non-cyclicsaturated hydrocarbon,

[0609] (425) 2-vinyl-4,4-dimethyl-2-cyclohexen-1-one

[0610] (426) 2-allyl-4,4-dimethyl-2-cyclohexen-1-one

[0611] (427) 4,4-dimethyl-2-isopropenyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0612] For example, when substituent R6 is cycloalkyl group of singlecyclic hydrocarbon,

[0613] (428) 2-cyclopropyl-4,4-dimethyl-2-cyclohexen-1-one

[0614] (429) 2-cyclobutyl-4,4-dimethyl-2-cyclohexen-1-one

[0615] (430) 2-cyclopentyl-4,4-dimethyl-2-cyclohexen-1-one

[0616] (431) 2-cyclohexyl-4,4-dimethyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0617] For example, when substituent R6 is allyl group of aromatichydrocarbon 1 valence group,

[0618] (432) 4,4-dimethyl-2-phenyl-2-cyclohexen-1-one

[0619] (433) 4,4-dimethyl-2-naphthyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified. Substituent R6 representsalkoxy carbonyl group and sometimes becomes ester.

[0620] For example, when substituent R6 is a hydroxy lower alkyl group,

[0621] (435) 4,4-dimethyl-2-hydroxy methyl-2-cyclohexen-1-one

[0622] (436) 4,4-dimethyl -2-hydroxy ethyl-2-cyclohexen-1-one

[0623] (437) 4,4-dimethyl -2-hydroxy propyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0624] For example, when substituent R6 is an amino lower alkyl group,

[0625] (438) 2-aminomethyl-4,4-dimethyl-2-cyclohexen-1-one

[0626] (439) 2-aminoethyl-4,4-dimethyl-2-cyclohexen-1-one

[0627] (440) 2-aminopropyl-4,4-dimethyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0628] For example, when substituent R6 is a lower alkylamino loweralkyl group,

[0629] (441) 4,4-dimethyl-2-methylaminomethyl-2-cyclohexen-1-one

[0630] (442) 4,4-dimethyl-2-ethylaminomethyl-2-cyclohexen-1-one

[0631] (443) 4,4-dimethyl-2-ethylaminoethyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0632] For example, when substituent R6 is a di-lower alkylamino loweralkyl group,

[0633] (444) 2-dimethylaminomethyl-4,4-dimethyl-2-cyclohexen-1-one

[0634] (445) 2-diethylaminomethyl-4,4-dimethyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0635] For example, when substituent R6 is cyclic amino group,

[0636] (446) 4,4-dimethyl-2-piperazinyl-2-cyclohexen-1-one

[0637] (447) 4,4-dimethyl-2-morpholinyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0638] For example, when substituent R6 is a cyclic amino lower alkylgroup,

[0639] (448) 4,4-dimethyl-2-piperazinylethyl-2-cyclohexen-1-one

[0640] (449) 4,4-dimethyl-2-pyrrolinylmethyl-2-cyclohexen-1-one

[0641] (450) 2-azethydinylmethyl-4,4-dimethyl-2-cyclohexen-1-one

[0642] (451) 4,4-dimethyl-2-morpholinylmethyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0643] For example, when substituent R6 is acylamino group ofmonoacylamin,

[0644] (452) 4,4-dimethyl-2-formylamino-2-cyclohexen-1-one

[0645] (453) 2-acetylamino-4,4-dimethyl-2-cyclohexen-1-one

[0646] (454) 4,4-dimethyl-2-propionylamino-2-cyclohexen-1-one

[0647] (455) 2-butyrylamino-4,4-dimethyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0648] For example, when substituent R6 is acyloxy group of ester,

[0649] (456) 4,4-dimethyl-2-formyloxy-2-cyclohexen-1-one

[0650] (457) 2-acetyloxy-4,4-dimethyl-2-cyclohexen-1-one

[0651] (458) 4,4-di methyl-2-propionyloxy-2-cyclohexen-1-one

[0652] (459) 2-butyryloxy-4,4-dimethyl-2-cyclohexen-1-one and so on, andthose acid addition salts are exemplified.

[0653] For example, when substituent R6 is a trihalogeno lower alkylgroup,

[0654] (460) 4,4-dimethyl-2-trichloromethyl-2-cyclohexen-1-one

[0655] (461) 4,4-dimethyl-2-trifluoromethyl-2-cyclohexen-1-one and soon, and those acid addition salts are exemplified.

[0656] For example, when substituent R6 is polycyclic group,

[0657] (462) 4,4-dimethyl-2-furyl-2-cyclohexen-1-one

[0658] (463) 4,4-dimethyl-2-propyl-2-cyclohexen-1-one

[0659] (464) 4,4-dimethyl-2-thienyl-2-cyclohexen-1-one

[0660] (465) 4,4-dimethyl-2-isoxazolyl-2-cyclohexen-1-one

[0661] (466) 4,4-dimethyl-2-imidazolyl-2-cyclohexen-1-one

[0662] (467) 4,4-dimethyl-2-thiazolyl-2-cyclohexen-1-one

[0663] (468) 4,4-dimethyl-2-pyrrolinyl-2-cyclohexen-1-one

[0664] (469) 2-benzofuryl-4,4-dimethyl-2-cyclohexen-1-one

[0665] (470) 2-benzothiazolyl-4,4-dimethyl-2-cyclohexen-1-one

[0666] (471) 2-pyridyl-4,4-dimethyl-2-cyclohexen-1-one

[0667] (472) 4,4-dimethyl-2-quinolyl-2-cyclohexen-1-one

[0668] (473) 4,4-dimethyl-2-pyrimidinyl-2-cyclohexen-1-one

[0669] (474) 4,4-dimethyl-2-morpholinyl-2-cyclohexen-1-one and so on,and those acid addition salts are exemplified.

[0670] For example, when R5 and/or R6 in chemical formula (3-b) are bondsubstituents of condensation polycyclic hydrocarbon compounds andcondensation heterocyclic compounds,

[0671] (475) 5H-4-dimethyl-7-oxo-indene

[0672] (476) 4-dimethyl-1-oxo-tetralin

[0673] (477) 3H-4-dimethyl-1-oxo-anthracene

[0674] (478) 5H-4-dimethyl-7-oxo-benzothiophene

[0675] (479) 5H-4-dimethyl-7-oxo-benzofuran

[0676] (480) 5H-4-dimethyl-7-oxo-indole

[0677] (481) 6H-5-dimethyl-8-oxo-quinoline

[0678] (482) 6H-5-dimethyl-8-oxo-quinoxaline

[0679] (483) 6H-5-dimethyl-8-oxo-cinnoline

[0680] (484) 5H-5-dimethyl-8-oxo-1,4-dithianaphthalene

[0681] (485) 3H-4-dimethyl-1-oxo-thianthrene, and those acid additionsalts are exemplified.

[0682] The compounds which is shown in chemical formula (1-a), (1-b),(2), (3-a) and (3-b) of this invention can be synthesized by the knownprocessing manners of organic synthesis with conventional organicchemical compounds and/or natural plant oils. When the acid additionsalts or the compounds which is shown in general formula (1-a), (1-b),(2), (3-a) and (3-b) are used as inhibitory or blocking agents offunction which is generated by multi-dimensional structure, it ispossible to be administered as a single agent or a combined agent withthe carrier substances which can be allowable as drugs. However, itneeds to be not restricted in the manner which is demonstrated in thisinvention. These compositions are dependent on routes and/or planning ofadministration.

[0683] When the acid addition salts or the compounds which is shown ingeneral formula (1-a), (1-b), (2), (3-a) and (3-b) are used as drugabove-mentioned, those can be administered orally or non-orally asmedicament compositions such as powders, granules, tablets, capsules,injection solutions by suitably mixing with adequate components such ascarrier substances, excipients or attenuants which are allowablepharmaceutically. Also, an effect of the compounds can be expected bymanner of vapor.

[0684] When the compound which is shown in chemical formula (1-a),(1-b), (2), (3-a) and (3-b) of this invention is used by oral route,several types of tablets, capsules, powder materials, granular agentsand liquid agents are available. When the compound is administeredthrough the non-oral route, those are used in the form of disinfectedfluid. When the compounds are used as types above-mentioned, the carriersubstances with nontoxic solids or fluids include in a composition.

[0685] As an example of solid carriers, capsules made by usual gelatinis used. Moreover, effective ingredients are utilized with subsidiarysubstances or by tabulating, granulating and/or powder packaging withoutsubsidiary substances. The following substances are used as theexcipients; gelatin, lactose, sugars such as glucose, cone, wheat, rice,starches such as corn starch, fatty acids such as stearic acid, fatbases such as calcium stearic acid and magnesium stearic acid, talc,vegetable oil, alcohol such as stearylalcohol and benzyl alcohol, gum,polyethylene alkylene glycol and so on.

[0686] These capsule, tablet, granule and powder are generally 0.1-80weight % and contains effective ingredient of 0.1-60 weight %. Liquidcarriers such as water, physiological saline, sugar solution, dextrosesolution, ethylene glycol, propylene glycol, glycols such aspolyethylene glycol, polyoxyethylene sorbitan monoolate are desirable.

[0687] When it is administered non-orally by the manner of intramuscularinjection, intravenous injection or hypodermic injection, the compoundsprovided in general formula (1-a), (1-b), (2), (3-a) and (3-b) are usedas the germ-free solution which is added other solutes such as mineralsor glucose in order to make the isotonic solution. Appropriate solventsfor an injection represent sterilizing water, solution of lidocainehydrochloride (for intramuscular injection), physiological saline,glucose solution, any kind of fluids for an intravenous injection,electrolyte solution (for intravenous injection) and so on. When thosesolutions for the injection are used, usual dosage is 0.01-20 weight %and is-desirable at 0.05-5 weight %.

[0688] In the case of liquids for oral administration, it is better tobe used as suspension or syrup with 0.01-20 weight %. A carrier of theseliquids is watery excipient such as perfume, syrup and micelle which areavailable for pharmaceutic manufacturing.

[0689] When the compounds in this invention are drug-manufactured bycombination with the carriers which is allowable on pharmaceutics,usually known methods and techniques are avairable. Concretely, whenointment, cream agents, emulsions or milky lotions are produced,silver-carried inorganic compounds, drugs and halogen compounds asoccasion demands are added at melting and mixing, simultaneously, duringand after emulsification resulting in ointments, cream agents or milkylotions. Also, drugs and/or halogen compounds can be added firstly. Whenthe compounds in this invention are used as sterilizing agents anddisinfectants for living space, an effect can be obtained by single useor combination with suitable carriers. Concretely, it makes operatedirectly or indirectly through a room air to solid surface by aspersion,embrocation or evaporation.

[0690] Also, a sterilizing effect can be obtained by adding thecompounds into water of humidifier and on any part of circulationcircuits of air-conditioning device. In addition, when the compounds inthis invention composition are used as depolymerization agents,improving agents for surface active substances, reductants, free radicalscavengers, desulfurization agents, phase transition agents, improvingagents of phase transition, improving agents of microphase separationstructure, promoting agents for plasticity and/or elasticity, improvingagent for plasticity and/or elasticity, copolymerization agents,copolymerization improving agents, polymerization regulators, improvingagents for polymerization adjustment, stabilizers, antioxidants,improving agents for crystallized materials and/or amorphous materials,flexibility promoters and/or improving agents for changing inflexibility, those compounds can effectively control, inhibit and/orgenerate an objective property of substances by using as a singlesubstance and/or a combination with adequate carriers. When thecompounds in this invention are used as modulators or improving agentsfor fluorescent wavelength and excitation wavelength of pigmentums,coating materials, cosmetic pigments or colorants, improving agents ofphysical property with low molecule substance, improving agents offunction with low molecule substance, improving agents of physicalproperty of macromolecules substance, improving agents of function withmacromolecules substance and/or improving agents of physical propertywith macromolecules composite materials and functional macromoleculescomposite materials, those compounds can effectively control, inhibitand/or generate an objective property with substances by using as asingle substance and/or a combination with adequate carriers.Concretely, an improvement of efficiencies can be planned by selecting amixing ratio with macromolecules substances, a churning temperature, anadjusting energy quantity such as protons and radio waves and/ortransition metals.

BRIEF DESCRIPTION OF THE DRAWINGS

[0691]FIG. 1 is a graph which represents the effect of Yoshixol, whichis a representative compound of inhibitory or blocking agents ofmolecular generating and/or inducing functions in this invention, onNADPH, NADP, heme and cytochrome C which were measured by a infraredspectrophotometer.

[0692]FIG. 2 is the graph which shows the effect of Yoshixol on aminoacids composition of human blood serum, thrombin and fibrinogen.

[0693]FIG. 3(a) and 3(b) is the graphs which show the effect of Yoshixolon blood coagulation measured by thromboelastgram.

[0694]FIG. 4 is the graph which was converted the digitalized data to agraphic design from stained contrast of electrophoresis which wasconfirmed the effect of Yoshixol on configuration and function ofproteins of trypsin and bovine albumin.

[0695]FIG. 5(a) and 5(b) are the graphs which show the effect ofYoshixol on serum antibodies for blood type judgment of ABO blood types,and which were converted the digitalized data to a graphic design from amagnitude of aggregated reaction.

[0696]FIG. 6 is the graph which shows an effect of Yoshixol on increasesin blood pressure due to vasopressin.

[0697]FIG. 7(a), 7(b) and 7(c) are the graph which was converted thedigitalized data to a graphic design from stained contrast ofelectrophoresis which was confirmed the effect of Yoshixol onconfiguration of proteins of bovine albumin and blood type anti-A bloodserum, anti-B blood serum.

[0698]FIG. 8(a), 8(b) and 8(c) are the graph which shows theantimicrobacterial effect of Yoshixol on methitilin resistancestaphylococcus aureus (MRSA), E. Coli or Candida albicans.

[0699]FIG. 9 is a picture of an scanning electron microscopy, whichdemonstrates a typical morphological aspect of the cell death of MRSAimmediately after treatment with Yoshixol.

[0700]FIG. 10 is a picture of an scanning electron microscopy, whichdemonstrates a typical morphological aspect of the cell death of E. coliimmediately after treatment with Yoshixol.

[0701]FIG. 11 is a picture of an scanning electron microscopy, whichdemonstrates a typical morphological aspect of the cell death ofacid-fast bacilli immediately after treatment with Yoshixol.

[0702]FIG. 12 is a picture of an scanning electron microscopy, whichdemonstrates a typical morphological aspect of the cell death of Candidaalbicans immediately after treatment with Yoshixol.

[0703]FIG. 13 is a picture of an scanning electron microscopy, whichdemonstrates a typical morphological aspect of the cell death ofpseudomonas aeruginosa immediately after treatment with Yoshixol.

[0704]FIG. 14 is the graph which shows the effect of Yoshixol on numbersof plaques formation of the bacteriophage infected to E. Coli.

[0705]FIG. 15 is the graph which shows the effect of Yoshixol on chickenmyeloblastosis virus (AMV) reverse transcriptase.

[0706]FIG. 16(a) and 16 (b) are histological pictures which show theeffect of Yoshixol on cultured keratinocytes, observed by a phasemicroscopy.

[0707]FIG. 17(a) and 17(b) are histological pictures which show theeffect of Yoshixol on cultured keratinocytes, observed by antransmission electron microscopy.

[0708]FIG. 18 is the graph which shows survival rate of the HeLa cellswhich were treated with Yoshixol.

[0709]FIG. 19 is a picture of an scanning electron microscopy, whichdemonstrates a typical morphological aspect of the cell death of HeLacells immediately after treatment with Yoshixol.

[0710]FIG. 20(a) and (b) are histological pictures which showmorphological changes of blood erythrocyte due to Yoshixol, observed bya scanning electron microscopy.

[0711]FIG. 21 is the histological picture that canine skin aftertreatment with Yoshixol was transplanted to rabbit, and that shows animplantable effect of rabbit skin as a donor to dogs as recipient whenYoshixol was treated intravenously after the transplantation.

[0712]FIG. 22 is a picture which shows a thrombolytic effect of Yoshixolon fresh thrombus.

[0713]FIG. 23 are graphs which show the effect of Yoshixol on change inamount of total proteins and concentration of serum albumin whenYoshixol was administered orally in dog.

[0714]FIG. 24 are graphs which show the effect of Yoshixol on change inamount of concentration of serum globulin and ratio of albumin vsglobulin when Yoshixol was administered orally in dog.

[0715]FIG. 25 are graphs which show the effect of Yoshixol on change intotal cholesterol and concentration of serum triglyceride when Yoshixolwas administered orally in dog.

[0716]FIG. 26 are graphs which show the effect of Yoshixol on change inserum nonproteins nitrogen and concentration of serum creatinine whenYoshixol was administered orally in dog.

[0717]FIG. 27 are graphs which show the effect of Yoshixol on change inconcentration of serum creatinine when Yoshixol was administered orallyin dog.

[0718]FIG. 28 are histological pictures which show the effect ofYoshixol on flagellum of bovine spermatozoa, observed by a scanningelectron microscopy.

[0719]FIG. 29 are histological pictures which show the effect ofYoshixol on flagellum of bovine spermatozoa, observed by a transmissionelectron microscopy.

[0720]FIG. 30 is a graph which shows a calorimetry effect of Yoshixol onpalmitic acid, measured by a digital scanning calorimeter.

[0721]FIG. 31 is a graph which shows a calorimetry effect of Yoshixol onpolyethylene glycol 1000, measured by a digital scanning calorimeter.

[0722]FIG. 32 is a graph which shows a calorimetry effect of Yoshixol onpolystyrene 280,000, measured by a digital scanning calorimeter.

[0723]FIG. 33 are graphs which show calorimetry effects of Yoshixol onmethyl methacrylate and ethyl methacrylate, measured by a digitalscanning calorimeter.

[0724]FIG. 34 are graphs which show calorimetry effects of Yoshixol onisobutyl methacrylate and poly (vinyl chloride), measured by a digitalscanning calorimeter.

[0725]FIG. 35 is a graph which shows a calorimetry effect of Yoshixol onpolyethylene glycol 4000 and poly (methylacrylate), measured by adigital scanning calorimeter.

[0726]FIG. 36 is a graph which shows a thermal mechanical effect ofYoshixol on poly (vinyl-chloride), measured by a thermal mechanicalanalyzer.

[0727]FIG. 37 is a picture of electrophoresis which shows the effect ofYoshixol on newly synthesized dimers with 7 base pairs.

[0728]FIG. 38 is a picture of electrophoresis which shows the effect ofYoshixol on PCR of snake DNA by using a newly synthesized dimer of 7base pairs as a primer.

[0729]FIG. 39 is a graph which shows the effect of Yoshixol on change inabsorbance of ethylene bromide, measured by a spectrophotometer.

BEST MODE FOR CARRYING OUT THE INVENTION

[0730] The chemical compound which is used and enforced in thisinvention is not especially limited. But, as one of a concrete andrepresentative compound which shows reasonable biological effect andwhich is easily synthesized chemically because of the simple chemicalstructure, it was synthesized4,4-dimethyl-6-methylene-2-cyclohexen-1-one (this compound is termed asYoshixol) which is the compound that all of substituent R3, R4, R5 andR6 shown in chemical formula (3-a) are hydrogen atoms. And, unlessotherwise specified, representative experiments are demonstrated usingthis Yoshixol so as to show the effectiveness of the present invention.Chemical formula of this compound is the following.

[0731] Yoshixol was synthesized according to the following processes.But, a synthesizing process of this compound is not restricted by thesynthesizing process which was demonstrated here.

[0732] To a solution of diisopropylamine (7.27 g, 7 mmol) in anhydroustetrahydrofuran (THF) was added drop wise a hexane solution (1.62 mol/l)of n-butyllithium (44.4 ml, 70 mmol) at −78° C. The solution was warmedto 0C and stirred for 1 hr at this temperature. After thus preparedlithium diisopopylamide solution was again cooled to −78° C.,4,4-dimethyl-2-cyclohexen-1-one (7.5 g, 60 mmol) was added dropwise andstirring was continued for 1 hr. Then, gaseous formaldehyde, generatedby a thermal decomposition of paraformaldehyde (5 g) over an oil bath,was blown through the solution with a gentle stream of dry nitrogen gasand the reaction mixture was stirred for 2 hr. After standing over nightat room temperature, 1N hydrochloric acid was added until the solutionbecame weak acid. The solvent was removed and the residue was extractedwith ether. After drying over anhydrous sodium sulfate and removal ofthe solvent, a mixture of 4,4-dimethyl- 6-methylene-2-cyclohexen-1-oneand 4,4-dimethyl- 6-hydroxymethyl- 2-cyclohexen-1-one was obtained (7.03g). This mixture (3.0 g) was treated in reflxing benzene for 2 hr in thepresence of catalytic amount of anhydrous p-toluenegulfonic acid andmolecular sieve 3A (4 g). The solution was neutralized with 1N sodiumbicarbonate and washed with brine. After drying over anhydrous sodiumsulfate and removal of the solvent, crude4,4-dimethyl-6-methylene-2-cyclohexen-1-one (Yoshixol) was obtained(2.35 g, overall yield 68%). The analytical sample was available.2-cyclohexen-1-one was obtained (2.35 g, overall yield 68%). Theanalytical sample was available after purification by columnchromatography or kugelrohr distillation but yield was much lowered.This NMR analysis of Yoshixol is following: IR(neat): 1670(C═O),1620(C═C) cm-1H NMR (60 MHZ, CCL4), d1.15 (s,6H,C(CH3)2), 2.57(bs,2H,CH2), 5.20, 5.93 (2m,2H,CH2=), 5.87 (d,J=10,1H,2-H), 6.63 (d,J=10Hz, 3-H).

[0733] <Stability of Solution Under Light>

[0734] Changes in coloring, viscosity and odor of Yoshixol into a sealedglass tube, which have been stocked under the room light, were observedat 6 months after the synthesis. As a result, those of fragrance,coloring and viscosity did not change and were identical to the initialproperty.

[0735] Though an effective dose of Yoshixol, the derivatives and thoseacid addition salts is blended, the adequate dosage differs dependentlyon body weights, administration routes, symptoms, individual patient orages and so on.

[0736] For example, when it is administered orally in adult patient,dosage of 0.01-5 mg/Kg weight per day, namely 0.1-2 mg/Kg of bodyweights per day, is acceptable and is divided into one or several timesa day.

[0737] And, when it is administered intravenously, dosage of 0.01-500mg/Kg body weight per day, namely 5-100 mg/Kg body weight per days isacceptable and is divided into one or several times a day. Moreover,when an objective to use in the life space so on is for a sterilizingand/or bactericidal action, a range of concentration between 0.5 and100picomole is desirable.

[0738] Though the following presentations by using Yoshixol aredemonstrated sequentially effectiveness of inhibitory or blocking agentsof the function induced or generated by multi-dimensional structurewhich is major points of this invention, Yoshixol is picked up as aconcrete and representative compound in order to most simply provideeffectiveness and basic mechanism. And also, the preparations andmethods of experiments which can most simply discuss the mechanism andwere most close historically toward the method of the original idea thathas been promoted to specialization in scientific world were chosen inthe invention. Therefore, the inhibitory or blocking agents of moleculargenerating and/or inducing functions which are provided in claims 1-6 ofthis invention are not restricted any more by experimental methods andregents demonstrated here. And, because this invention consists of planswhich are able to provide and discuss above-mentioned biological effectsfrom a respect with physical property of substances, this inventionprovides effectiveness on low molecule substances and macromoleculessubstances of non-living organism as shown in representative examples.

[0739] Though the following presentations by using Yoshixol aredemonstrated sequentially effectiveness of controlling, inhibitoryand/or blocking agents of the function induced or generated bymulti-dimensional structure of low molecular substances and/ormacromolecular substances in this invention, Yoshixol is picked up as aconcrete and representative compound in order to most simply provideeffectiveness and basic mechanism, identically in the case of biologicaleffects. And also, the preparations and methods of experiments which canmost simply confirm the mechanism were chosen in the invention.Therefore, the inhibitory or blocking agents of molecular generatingand/or inducing functions which are provided in claims 1-11 of thisinvention are not restricted any more by experimental methods, regentsand analysis demonstrated here.

[0740] <Concerning to Reactions with Ribose, Glycerin, Cellulose andPolyethylene Vinyl>

[0741] Each 1 ml of glycerin, cellulose, polyethylene vinyl and ribose(1 mol) was mixed respectively with 4 μl of Yoshixol in the test tubeand ways blended. Then, a fluidability and transparence of the reactedsubstance in each sample tube were investigated at room temperature (28°C.), heating (80° C.) or cooling (4° C.) state. At room temperature,transparence and softness of each sample in test tube increased. Wheneach sample was cooled, increases in hardness and cloudy occurred. Incontrast, at high temperature, increases in fluidability andtransparence of each sample occurred to be enhanced greater than abovetwo conditions. This result shows that Yoshixol has polymerizationand/or depolymerization effect.

[0742] <Effect on NADPH, Heme and Cytochrome C>

[0743] Changes in concentration of NADPH (340 nanometer), cytochrome C(415, 520, 550 nanometer), heme (415 nanometer) and aromatic amino acids(280 nanometer) in 1 μl of defibrinized human blood serum were measuredbefore and after treatment with 4 μl of Yoshixol by an infraredspectrophotometer. Subsequently, although concentration of NADPH,cytochrome C and heme did not alter even after treatment with Yoshixol,characteristic peak of wave length with amino acids was disappeared andshifted to lower wave length (range of aromatic amines). The resultshows that Yoshixol has an effect of producing new aromatic amines notonly due to dehydrogenation but due to reduction and/or hydrogenbinding. FIG. 1 shows that extremely high and monophasic peak of wavelength occurred resulting from disappearance of biphasic peak increasedat 280 nanometer.

[0744] <Effect on Composition of Amino Acids in Human Blood Serum,Fibrinogen and Thrombin>

[0745] Changes in composition of amino acids were analyzed by use of 1ml of human blood serum, 1 ml of human fibrinogen (concentration of 160mg/dl), 1 ml of human thrombin before and after treatment with Yoshixol(4 μl). The total amino acids in the human blood serum which was treatedwith Yoshixol decreased by 41%. And, ratio of each composition wasaltered after the treatment so that as an example the concentration ofphosphoserine increased about 20 times which level was from 7.2 picomoleto 164.8 picomole. Moreover, though concentration of the total aminoacids in fibrinogen did not change by treatment with Yoshixol, glutamicacid and hydroxyl serine which were existed before treatment weredisappeared after the treatment and, concentration of cystathione infibrinogen increased to level of more than 5 times. In addition, inthrombin sample which was treated with Yoshixol, glutamic acid, taurine,methionine and aminoisobutylic acid which did not exist before thetreatment were produced newly. This result shows that Yoshixol has aneffect of a cross-linking coupling such as desulfurization reaction andhas an effect which can change from proteins and molecule of amino acidsto other molecular configurations of amino acids.

[0746] <Effect on Human Blood Coagulation and Fibrin Formation>

[0747] Effect of Yoshixol (4 μl ) on human blood coagulation and fibrinformation (thrombin was added to fibrinogen) were investigated bythromboelastgram (Hellige GMBH, West Germany). Also, a magnitude offibrin network which is formed at human blood coagulation wasinvestigated by a scanning electron microscopy. Coagulation of humanblood without treatment with Yoshixol was started within 1-2 min so thatmaximum level of coagulation occurred approximately within 15 min,followed by gradual decrease due to activation of fibrinolytic system.Immediately after thrombin is added on fibrinogen, viscosity of thesample started to increase, reached to a maximum level within 5-6minutes. This maximum level was maintained for periods of 6 hours whichwas observed (referred FIG. 3a). However, when Yoshixol (4 μl) was addedin 0.4 ml of whole blood or fibrinogen (160 mg/dl), onset time of bloodcoagulation and fibrin formation was delayed to 4-5 minutes and maximumaggregation time was occurred within 6-8 minutes. Maximum level ofcoagulation after the treatment was inhibited by 90% of control whichlevel was maintained over 6 hours of investigation (referred FIG. 3b).And, when thrombin treated with Yoshixol was added in fibrinogen, any ofaggregation reaction was not be found on thromboelastgram. Moreover, inmorphological investigations of blood coagulation, rouleaux formation oferythrocyte and formation of fibrin net occurred markedly in thenon-treated group with Yoshixol, however, those formations in treatedgroup with Yoshixol did not occur. The result shows that Yoshixol has astrong anticoagulant effect (anti-thrombin effect) and antifibrinolyticeffects.

[0748] <Effects on Change in Function of Trypsin and Thrombin and on itsConfiguration Change>

[0749] Each physiological effect of trypsin (Wakou Jyunyaku Ltd.) andthrombin (Behlinger Manheim-Yamanouchi Co.) was investigated byelectrophoresis. When trypsin was added to bovine albumin (Sigma Co.Saint Louis, Mo., USA) or myoglobin (Sigma Co. Saint Louis, Mo., USA),each primary structure of proteins which consist of albumin was alteredby proteolytic action of trypsin. In addition, when thrombin was addedto human fibrinogen (Behlinger Manheim-Yamanouchi Co.), a primarystructure of proteins which consists of fibrinogen was not found.Moreover, primary structure of proteins which consist of trypsin orfibrinogen did not show any electrophoretic changes even after treatmentwith Yoshixol (4 μl) and, physiological function of trypsin orfibrinogen to bovine albumin, myoglobin and fibrinogen did not occur(referred FIG. 4). This result shows that Yoshixol can block specificityof function which each trypsin or thrombin has because of changingmulti-dimensional structure, but not of changing primary structure oftrypsin or thrombin.

[0750] <Effect on Function of Serum Antibodies for ABO Blood Types>

[0751] It is also known that antibody has a structure of Y shape whichconsists of 2 pairs of light chain and heavy chain in generally, andthat the fundamental structure is maintained by S-S bond. Serum antibodyreaction of ABO blood types is important historically to understandvarious kinds of antigen-antibody reactions. In this invention, effectof Yoshixol (4 μl) on the standard judgment of ABO blood types wasinvestigated by using human blood of A type, B type and 0 type (400 μl,respectively ). When each antiserum of blood types was not treated withYoshixol, antiserum could judge blood type ordinally, resulting fromthat anti-A blood serum caused a blood aggregation when it was added tohuman blood of A type, anti-B blood serum caused a blood aggregationwhen it was added to human blood of B type and both of anti serums didnot cause blood aggregation when it was added to human blood of 0 type(referred FIG. 5a). But, when a judgment of ABO type blood type was doneby using each antiserum treated with Yoshixol (4 μl), any aggregationdid not occur in sample blood with each blood type, and normal judgmentof ABO blood type was impossible (referred FIG. 5b). Moreover, when aprimary structure of antiserums for ABO blood types was investigated byan electrophoretic analysis, any change in primary structure ofantiserums did not find even after treatment of Yoshixol. Thus, theresults show that Yoshixol can inhibit or block an antibody functionwhich is induced or generated by multi-dimensional structure more thanprimary structure of antibody.

[0752] <Effect on Physiological Function of Vasopressin and Insulin asPeptides>

[0753] Each vasopressin and insulin has a physiological effect such as arise of blood pressure and a fall of sugar level in blood respectively.An effect of Yoshixol on these physiological functions was investigatedand compared by injection of each hormone without or with treatment withYoshixol in rabbit in vivo. When vasopressin (100 ng/Kg, Sigma Co. SaintLouis, Mo., USA) without treatment with Yoshixol was injectedintravenously, blood pressure increased by 15-25 mmHg so that thisincreased level was maintained for about 25 minutes. But, vasopressin(100 ng/Kg) treated with Yoshixol (4 μl) caused a increase in bloodpressure of only about 5 mmHg (referred FIG. 6). Moreover, a maximalfall of blood sugar level due to injection of insulin (5 units/Kg, NovoLtd.) without treatment with Yoshixol was 45 mg/dl. When insulin treatedwith Yoshixol (4 μl) was injected, change in blood sugar level was only12 mg/dl. The results show that Yoshixol can inhibit or blockphysiological effect on bioactive peptides with low molecule andhormones which have functional specificity consisted and generated byamino acid sequences.

[0754] <Effect on Primary Structure of Proteins>

[0755] Changes in molecular weight composition of the followingmacromolecular proteins (1 mole solution) before and after treatmentwith Yoshixol (4 μl) were investigated after heated denaturation byelectrophoretic analysis of non-SDS wide page. The used macromoleculesproteins solutions of 1 ml are human defibrinized serum, bovine albumin,human fibrinogen, myoglobin, anti-A blood type serum and anti-B bloodtype serum (Green Cross Co.). Even after treatment with Yoshixol,distribution of molecular weights on electrophoretic analysis wasidentical to that of the macromolecules proteins which is not treated(referred FIG. 7). This result shows that Yoshixol does not directlychange a primary structure of a biological proteins with macromoleculesbecause of an identical pattern of electrophoretic analysis of eachnon-treated sample with Yoshixol.

[0756] <Concerning about Anti-Microbacterial Effects>

[0757] (Effect on methitilin resistance staphylococcus aureus, MRSA)Effect of Yoshixol on MRSA was investigated by using the original strain(stock no. SCK18,) which was isolated from sepsis patient and which wasconfirmed to cause severe circulatory shock in experimental animals suchas mouse, rat, rabbit and dog. Culture medium was used a brain-heartinfusion agar. Using dosage of Yoshixol between 0.25 μl and 10 μl per 1ml of culture medium, colony formation unit (CFU) was measured after24-hour incubation at 37° C. and the initial CFU was 10⁸. CFU innon-treated group with Yoshixol as control group increased to 10¹⁰during 24-hour cultured, however, CFU in treated group with Yoshixol(0.25 μl per 1 ml of culture medium) decreased to 10⁴. Additionally, atdosages of 2 μl and 10 μl of Yoshixol per 1 ml of culture medium CFUwere 10² and zero respectively (referred FIG. 8a). The result show thatYoshixol has a strong bactericidal effect on MRSA which has beenacquired resistance to other antibiotics in gram positive bacteria.

[0758] (Effect on E. Coli) Effect of Yoshixol was investigated by usingE. Coli (E. coli strain no. W3110) and brain-heart infusion agar asculture medium. Using dosage of Yoshixol (2 μl per 1 ml of culturemedium), colony formation unit (CFU) was measured after 24-hourincubation at 37° C. and the initial CFU was 10⁸. CFU in non-treatedgroup with Yoshixol as control group increased to 10¹⁰ during 24-hourcultured, however, CFU in treated group with Yoshixol (2 μl per 1 ml ofculture medium) decreased to zero after 1 hour cultured, and was stillzero after 24 hours (referred FIG. 8b). The result show that Yoshixolhas an extremely strong bactericidal effect on E. coli which is gramnegative bacteria.

[0759] (Effect on acid-fast bacteria) Effect of Yoshixol wasinvestigated by using atypical mycobacteria (Mycobacterium Rapid Grower)and judged the effect by measuring a size of inhibition zone ofproliferation on brain-heart infusion agar. The formation of inhibitionzone of proliferation occurred at 0.2 μl of Yoshixol per 1 ml of theculture medium and revealed 22 mm of the diameter at 2 μl. The resultshows that Yoshixol has a strong bactericidal effect on atypicalmycobacteria.

[0760] (Concerning about antifungal effect) In order to investigateeffect of Yoshixol (2 μl per 1 ml of culture medium on Candida albicans,it was investigated by using Candida Albicans (10⁶ CFU/ml) and Sabouraudbroth (5 ml). In non treated group with Yoshixol, CFU did not changeafter 3 hours incubated, and tended to increase. However, in treatedgroup with Yoshixol, CFU became zero after 1 hour. This level of zerowas maintained even after 3 hours incubated. This result show thatYoshixol has an strong antifungal effect.

[0761] Those antibacterial effects provide interests related tohistological aspect of cell death. Thus, in MRSA, investigation by ascanning electron microscopy showed characteristic histological imagesafter Yoshixol that grouped MRSA bacilli was separated to an individualbacterial cell, and that small particles with a size of 10-50 nm weresprayed out with an explosive aspect from surface structure of theindividual cell (FIG. 9) and, that as at the final stage of cell deaththe smaller particles than the above were dispersed like fireworks withconcentric circle. Such characteristic aspects were also observed by atransmission electron microscopic image. Scanning electron microscopicobservation of E. Coli showed that the surface of E. coli were loosedthe smoothness and were consisted of small particles about 10-50 nm and,that some expanded prominences were appeared on the surface (referredFIG. 10). In the case of E. coli, of course, an adhesive group ofbacilli lost and the products at the final stage were destroyedresulting in small particles. Even in cases of acid-fast bacteria(referred FIG. 11) and Candida albicans (referred FIG. 12) aftertreatment with Yoshixol, similar histological aspects were observed.Moreover, histological observation of pseudomonas aeruginosa aftertreatment with Yoshixol showed that the bacilli were swelled as likelyas a balloon and were ruptured so that components of the bacilli becameinto small particles (referred FIG. 13). These results show that thoughYoshixol has a disinfective and antimicrobacterial effect, mechanism forcell death differs from the antibacterial and bactericidal mechanismwith conventional drugs such as denaturation, necrosis and/orcoagulation. The characteristic mechanism related to effect of Yoshixolon microbacteria is to inhibit an adhesion between individual bacteriaand to produce small particles by destroying the components of bacilli,with an aspect of erupting, explosing and/or ballooning according tomolecular composition which is contributed to each morphogeneis ofbacilli. These histological findings are identical with zeiosis orapoptosis which has been pointed out. Thus, this indicated point showsthat it is possible to apply Yoshixol as effective antibacterial and/orbactericidal agents which do not induce a variability anddrug-resistance

[0762] <Concerning to Disinfection Sterilizing Effect>

[0763] In order to investigate antimicrobacterial effect of evaporatingcomponent of Yoshixol, antimicrobacterial effect of Yoshixol in thisinvention, which concentration is 50 μl in the whole space of theschale, was studied by culturing the bacilli of methitiline resistancestaphylococcus aureus, E. Coli, Candida albicans and acid-fast bacteriawhich were same strains mentioned above in the ordinary gelatin agar andBHI (brain heart infusion) culture medium, heart infusion culture mediumand Sabouraud culture medium. It was done to investigate prolifelationof each bacteria during 24 hours incubation by avoiding to contact withculture medium which was disseminated each bacteria and a piece offilter paper which was dipped in adequate amount of Yoshixol. For it,the position of culture medium was upside and sample paper was put onthe base of the schale. Subsequently, proliferation of each bacteriamentioned above did not occur even at indirect contact due toevaporating component of Yoshixol from the base of the schale in aconstant-temperature state of 37° C., but not due to a direct contactdiffusion. This result shows that volatilizating and/or evaporatingcomponent of Yoshixol in this invention comfirmatively has a strongeffect as bactericidal and/or sterilized agent even when it is used viaroom air in the living space.

[0764] <Concerning Effect on Production of Nitric Oxide>

[0765] Recent interest has been focused recently in effects of nitricoxide (NO) which is generated in body. Such effects are anticancereffect, bactericidal effect, inhibitory effect of antigen-antibodyreaction and cardiovascular effect. Involvement of NO in the effects ofYoshixol which was demonstrated above, such as effect on bloodaggregation, effect on fibrin formation and antibacterial effect onMRSA, was investigated by using NG-methyl-L-arginine (NMLA) as blockingagent of generating NO. When 4 μl of NMLA (1 mol) was added in the eachtest sample with and without Yoshixol, blood aggregation effect, effectof fibrin formation and bactericidal effect of Yoshixol were decreasedby 10-20% comparing to effect of Yoshixol alone. This result shows thatYoshixol is a NO producing agent in vivo and that the produced NO byYoshixol contributes to about 10-20% of anticancer effect, bactericidaleffect, anti-viral effect and effect on antigen-antibody reaction ofYoshixol.

[0766] <Effect on Bacteriophage>

[0767] Yoshixol (4 μl) were added in 1 ml of phage solution (E79double-chained DNA phage) which was adjusted on about 10⁷ per 1 ml, andwere mixed well. Then, 10 μl of the mixture sampled after 5, 10, 20, 30minutes was diluted by quickly adding in 10 ml of medium, so that 100 μlof the phage-diluted solution put into the test tube as the upper platewith the warmed gelatin agar, which was mixed with 100 μl of theindication bacterial solution (pseudomonas aeruginosa) cultured for onenight. Then, the adjusted solution of the phages in the test tube wasdropped on the agar plate and, homogeneous surface of the upper agarplate was produced by smoothly rotating the plate on the table. Afterresting it on the table about 10 minute when multilayer gelatin agarsufficiently became solid, they were stocked into the incubator at 37°C. After one night incubation, numbers of plaques were counted. As aresult, the numbers of plaques in the 5 min-treated phage solution, in10 min-treated phage solution and in the 15 min-treated phage solutionwith Yoshixol decreased to 33%, 15% and 6% of the plaques formation inthe non-treated phage solution, respectively. Moreover, when the phagesolution was treated with Yoshixol over 20 min, plaques formation didnot find (referred FIG. 14).

[0768] <Concerning Antiviral Effect>

[0769] In order to investigate the effect on virus, changes in structureof single strand DNA, double strand DNA and mRNA of E. colibacteriophage (1 ml of 1 mol solution), which were prepared asnon-treated sample and treated sample with 4 μl of Yoshixol, wereobserved by scanning and transmission electron microscopes. In addition,according a general bacteriological technique, changes in proliferationand in morphological aspect (by scanning and transmission electronmicroscopes) of E. Coli, which was infected by single strand DNA, doublestrand DNA or mRNA, were investigated before and after treatment of eachphage with Yoshixol. As treated samples, 4 μl of Yoshixol was added in 1ml of each phage solution which concentration was adjusted to 1 mol. Asa result, a characteristic helical and multi-dimensional structure withsingle strand DNA, double strand DNA and mRNA of E. Coli bacteriophagebecame a simple structure after treatment with Yoshixol and, a distanceof the chain was markedly separated. On histological investigation of E.coli, an adhesion of the phage on the bacterial surface and/orintrabacterial existence were observed in the non-treated group, but notin the treated group with Yoshixol. In addition, an effect of Yoshixolon chicken myeloblastosis virus (AMV) reverse transcriptase (Gibco Co.Getesburg, Md., USA ) was investigated by measuring amount of cDNAsynthesis, which was amplified by PCR of RNA(5 μg) and AMV reversetranscriptase (25 units). As treated group, 0.01 μl of Yoshixol wasadded to 25 units sample of the AMV reverse transcriptase. Thus, theexpected production of cDNA was obtained in the non-treated group,however, the amount of cDNA production decreased to 10% of the expectedone when Yoshixol was treated (referred FIG. 15). This result shows thatYoshixol has inhibitory effect for self prolifelation ability withinhost cells, destroying action of virus, inhibitory effect for adhesionwith host cells, and effect which causes a change in multi-dimensionalstructure of genes with virus oneself.

[0770] <Concerning Anti-Cancer Effect>

[0771] Adhesive factors between cells play an important role onprolifelation of malignant tumor cells and metastasis. In order toinvestigate the adhesive factors between cells, intracellular structureof cultured keratinocytes are utilized to observe. Thus, by usingkeratinocytes isolated from a human skin and cultured in this invention,structure between cells and cellular aspect of keratinocytes (5 dayspassed after culturing of second generation) were investigated by phasemicroscope (Olympus Co., IMT-2), transmission type (JEOL, Ltd. JEM 1200,EXII) and scanning type (JEOL, Ltd. JSM-6000F) electron microscopes. Inthe non-treated group with Yoshixol, the cultured cells proliferatedmonologously and in order as like as a stone wall. There were normalaspects of intracellular organella and mitosis. There were not blankspaces between cell and filling with intracellular matrix (referred FIG.16a, 17 a). In contrast, aspects of cultured cells in the treated groupwith 4 μl of Yoshixol showed diverse irregularity. Moreover, there weremany cells which cell membrane and intracellular organella (Goljiapparatus, rough endoplasmic reticulum, cytoskeleton which consists oftubulin) were destroyed with varieties and coupling between cells hasalso estranged in an irregularity. In addition, extracellular matrix hasbeen also dispersed in an irregularity from cells as various sizes ofparticles (referred FIG. 16b, 17 b). These observations similar to theabove were found in cultured HeLa cells (American Type CultureCollection, ATCC No. CCL2, Maryland, USA, referred FIG. 18) and culturedmouse hepatoma cells. This result shows that Yoshixol in this inventioncan suppress cell division and prolifelation, and can block adhesionbetween cells. And also, Yoshixol has an inhibitory effect of cellprolifelation and metastasis such as tumor cells. Additionally, fromhistological findings, aspects of destroyed cells due to Yoshixol is farfrom those of necrosis in cell death which has been reported (referredFIG. 19) and, is more close to the picture which have been reported asnatural cell death or apoptosis (these morphologic images wereinvestigated in various bacteria mentioned above). And also, thesefindings show that-small particles destroyed from cell composition(10-100 nm) were cleaned up by phagocytosis of macrophages and/orlymphocytes, resulting in reuptaking those particles and being recyclinginto the natural physiological phenomena of living organism.

[0772] <Concerning Preservative Effect on Organs and Tissues>

[0773] After sampling 5 ml of human blood from a cubital vein, the bloodsample was replaced into the vacuum tube with 10 ml capacity and wasmixed in a gentle. The vacuum tubes were divided by two group; one groupis nontreated and another treated with 4 μl of Yoshixol. Then, changesin morphological aspects of blood, which were stored at roomtemperature, were observed by a transmission type and scanning electronmicroscopes at 30 minutes, one hour and 1 month after the sampling. Whenthe blood sample was not treated with Yoshixol, coagulated masses werefound 30 minutes after the sampling and, normal aspects of erythrocytesdid not found. It was existed likely as a destroyed and aggregated mass.However, erythrocytes which were processed by Yoshixol did not show anaggregation with fibrin networks. Many stomatocytes (lip-likeerythrocyte) and echinocyte which is appeared at a lack of pyruvatekinase were observed. However, cell membrane and intracellular organellawere preserved normally over 1 month (referred FIG. 20). This resultshows that blood treated with Yoshixol can be stored even in roomtemperature and has an effectiveness as preservative agents for organsand tissues which are functional units of body.

[0774] <Concerning Inhibitory Effect of Rejected Reaction onHeterogeneous Skin Implantation>

[0775] Changes in transplanted skin for 3 months were observed bymacroscopically and microscopically, when a piece of skin with entirelayer (diameter 3 centimeter meter) at a region of the back of rabbitwas transplanted to the region of the back of adult mongrel dog as theentire layer transplantation, and when a piece of skin with entire layer(diameter 3 centimeter meter) at a region of the back of adult mongreldog was transplanted to the region of the back of rabbit as the entirelayer transplantation. Firstly, each piece of skin from rabbit or dogwas treated with 5 ml of physiological saline with 10 μl of the testsolution for 2 minutes so that each skin piece was transplanted to eachrecipient by the surgical suture. Two kinds of the test solution wereprepared for the above treatment; as control solution, basal solutionconsists of 2 ml of polyoxyethylene (20) sorbitan monoolate 1 (WakouJyunyaku Co. ) which is identical to Tween 80 (ICI Ltd.) and 88 ml ofphysiological saline, and as treated solution, 10 ml of Yoshixol wasadded in the basal solution. And, 10 μl of Yoshixol was treated directlyon the transplanted wound for 3 days after implantation. Desquamation ofeach transplanted skin which were treated with the basal solution ascontrol group began on 3-5th days after implantation, and thetransplanted wound showed extremely dirty aspect with tissue necrosisand inflammation reaction. After one week, the transplanted skin showedmummification so that it was dropped out from the recipient completely10 days after the implantation. Then, implantated wound of the recipientwas cured with a self regenerated skin of each recipient after 3 months.On the other hand, when a piece of transplanted skin is dipped in theYoshixol solution, the treated skin became to be soft and increases init's thickness. And, a suture procedure with surgical needle was easilydone. The transplanted skin did not show a,desquamation and deciduation2 weeks after the implantation, and an inflammation reaction also wasinhibited. So that an inflammatory tissue reaction was not also foundafter 1 month. The transplanted wound showed an aspect which was coveredwith chitin-like and lustered collagens-like substances so that thewound was cured to a level which could not find a boundary with a skinof recipient (upper panel of FIG. 21). These results show that Yoshixolcan inhibit a rejection reaction for the transplantation by pretreatmentof tissues or organs of donor with Yoshixol when heterogeneoustransplantation of tissues or organs as well as skin was performed.Simultaneously with the above, Yoshixol can inhibit complications ofinfections on the donor tissues or organs, and can improve animplantation effect. Moreover, by using an entire layer (diameter 3centimeter meter) of rabbit skin, changes in a piece of the transplantedskin which was sutured to the back of the dog as the recipient wereinvestigated over 3 months after the implantation. The rabbit skin didnot receive the pretreatment with Yoshixol. The recipient dogs werereceived 10 μl/Kg per day of Yoshixol intravenously for one week, andthey did not receive any kinds of conventional antibiotics and/orimmunosuppressants. It was found that an transplanted skin was implantedon the back of dog over 1 month without a rejection reaction andbacterial infection. An outer layer of the transplanted skin was faded 3month after the implantation likely as to strip a thin membrane. But,though an appearance of a hair was not found in a wounded skin, wellepithelialization was found macroscopically and microscopically (lowerpanel of FIG. 21). In addition, by this intravenous administration ofYoshixol, adult mongrel dog also became vigor, youthful andappetite-well in comparison with behaviors-before the treatment. Thisresult shows that Yoshixol can inhibit a rejection reaction of thetransplantation as well as an improvement of physical status due to theintravenous administration. And, it can also simultaneously inhibitinfections and can improve an implantation effect.

[0776] <Concerning Thrombolytic Effect>

[0777] In order to investigate a thrombolytic effect of Yoshixol onthrombus, 1 ml of human blood or canine blood were sampled by a syringeand transferred into the Petori-schale (grainer lab. GmHB) so thatthrombus formation and rouleaux formation were observed under a phasecontrasted microscopy (IMT-2, Olympus Co.). Then, 1 μl of Yoshixol wasadded in the blood sample when all visual fields could not bediscriminated as an normal individual erythrocyte by thrombus formation.Then, a thrombolytic process of the thrombus was investigated and theprocess was recorded to a video tape via a collar video camera(CCD-IRIS, Sony Co.). The video pictures were analyzed as a liquidphenomena by an original software of dynamic state analysis. WhenYoshixol was added in the sample, the thrombus which has consisted witha mass has completely individualized to each erythrocyte via a reversedprocess of the thrombus formation. And, while original form oferythrocyte was recovered, each erythrocyte was marvelously dispersedfrom thrombus. In addition, hemolysis due to swelling and rupturing eacherythrocyte did not occur. Each position of the individual erythrocytedid not disturb a position of other erythrocyte, and as a whole therewas a dynamic state with a defined order (referred FIG. 22 ). On beinganalyzed this process by a dynamic image processing or microscopically,the pattern of this process showed a behavior as a dissipative masssimilarly to phenomenon of liquidarization of solid materials orgelatinization phenomenon. This result show that mechanism ofthrombogeneis in the blood and serum which is one example ofnon-newtonian physical property is interpreted by thermodynamically.And, Yoshixol has a potential to improve circulatory hindrance which isdisturbed physiological role on original blood such as fluidability bybeing solidability. Yoshixol can apply as thrombolytic agents as well asinhibitory agents for thrombus formation.

[0778] <Concerning Effect on Improving Metabolism>

[0779] In order to investigate changes in blood cells, chemicalcomponents in blood and improving effect on metabolism after oraladministration of Yoshixol, 10 μl per body weight of Yoshixol was mixedwith 100 g of dog foods (“dog foods <beef>”, produced in New Zealand,imported by Daiei, Inc., followed by pet food fair trading committeestandard), this food was given to the beagles as their feedstuff. Oraladministration was continued for 1 week, and samplings of blood wasperformed before, 1 day after and 3 day after administration, and 1 dayafter and 7 days after the stop of the administration. And, red bloodcells, white blood cells and platelets were counted. Also, totalproteins (Byuret method) in a blood serum, albumin (BCG method), ureanitrogen (GLDH-UV method), creatinine (enzymic method), glucose (GDHmethod), total bilirubin (enzymic method) are measured. GOT and GPT(JSCC sub method), TTT and ZTT (standard method of research project ofliver function), cholinesterase (DMBT method), total cholesterol (PDOenzymic method), triglyceride (PDO enzymic method), uric acid (urikasePDO method), serum iron (nitroso PSAP method), creatinine phosphokinase(SCC sub method), sodium, potassium and chloride (ISE dilution),inorganic phosphorus (enzymes-UV method) and calcium (OCPC method) werealso measured. As a result, any changes in numbers of red blood cells,white blood cells and platelets did not found. Moreover, any changes inconcentration of total bilirubin, GOT, GPT, TTT, ZTT, cholinesterase,serum iron, potassium, sodium, chloride, inorganic phosphorus andcalcium did not found. However, total proteins increased 3 days afteradministration of Yoshixol followed by recovery to a same level in thecontrol 1 week after the stop of administration. Though albumin leveldid not change (referred FIG. 23), albumin/globulin ratio was elevated 3days after administration (referred upper panel of FIG. 24) indicatingof newly producing globulin. Moreover, though blood sugar level waselevated by 15% of the control group 3 days after taking feedstuff, thiselevated blood sugar level did not found in the treated group withYoshixol and the rebound phenomena of the glucose metabolism did notoccur 1 week after the stop of administration (referred lower panel ofFIG. 24). A difference in concentration of total cholesterol andtriglyceride between groups did not occur (referred FIG. 25). But,levels of nonproteins nitrogen and creatinine in the serum showed lowervalue (70-80% of the control) since 1 day after administration (referredFIG. 26), and level of uric acid also was maintained at lower levelduring the administration. In addition, creatinine phosphokinase fell(referred FIG. 27), and enzymes such as γ-GPT, GOT, GPT also fell. TTTand ZTT did not show abnormal values. During this administration ofYoshixol and 1 weeks after stopping administration, any abnormalbehaviors, diarrhea, vomiting and bloody feces, loss of the weight andappetite loss were not observed. Moreover, even though 3 μl per bodyweight of Yoshixol was administered for one month to the beagles and theparameters of blood samples were observed during 3 months, a similareffect of Yoshixol to the above experiments could be obtained eventhough there was a difference of the time-lag and a degree. Theseresults show that oral administration of Yoshixol can be expectedseveral effects to improve metabolism and nutrition such as saccharides,lipids and proteins. Thus, Yoshixol can apply as therapeutic drugs intoprotective agents for cellular function as well as agents for diabetes,kidney diseases, heptic diseases and hypoproteinsemia.

[0780] <Concerning Softening and Flexibility Effect on Skin>

[0781] In order to investigate changes of softening and flexibility onskin from rabbit and dog, each skin was is dipped in 5 ml ofphysiological saline with 10 μl of the test solution. This test solutionwas prepared from 88 ml of physiological saline with 2 ml ofpolyoxyethylene (20) sorbitan monoolate 1 (Wakou Jyunyaku Co.) that isidentical to Tween80 (ICI Co.) as the basal solution of control. As thetreated solution, 10 ml of Yoshixol was added in the basal solution.When each skin sample was dipped in the test solution for approximately1-2 minute, the treated skin became soft, wetly and thicken. Surgicalstitching by the needle was easily to be inserted and transfixed in theskin. Additionally, structure damages of each skin did not foundhistologically. And, the sample treated with Yoshixol was observed asthe preparation which was made from a fresher sample by hematbxylineosin staining in contrast to the skin sample treated with the testsolution of control. Moreover, a similar observation on histologicalpictures of each sample was obtained even when each skin sample wasthawed at 20° C. after storaging each sample at 4° C. in therefrigeration for one month. This result shows that it is possible thatYoshixol can apply as flexibility promoters and/or softners of thetissues and/or substances which have fiber structures such as skin and,that Yoshixol can utilize as preserving agents for organs.

[0782] <Concerning Inhibitory Effect on Flagellum Motility ofSpermatozoa>

[0783] In order to investigate an effect of Yoshixol on a flagellummotility of spermatozoa, the spermatozoa (seed japanese bull ID:Sinmorihide <registration No. Zen-Wa-Kuro1114, lot No.84Y28>) which hasbeen conserved in the liquid nitrogen was thawing at 35° C. Afterthawing, 1 ml of semen was transferred to Petori-schale (grainer lab.GmHB) and, flagellum motility was observed by a phase contrastmicroscopy (IMT-2, Olympus Co.) and was recorded by a video film via acollar video camera (CCD-IRIS, Sony Co.) so that wave cycles and speedof the flagellum were analyzes by an original software of dynamic stateanalyzer. While a head of normal spermatozoa was transferred by regularmovement of a flagellum at the speed of 0.3-1.5 mm per second, aflagellum movement was immediately inhibited after 1 μl of Yoshixol wasadded so that velocity of spermatozoa became zero. However, though aflagellum movement was completely stopped, the rotation of the headwhich occurs at the centriole (near junction between head and tail) wasfound during a few 10 seconds. And, a speed of this rotation graduallywas decelerated with progress of a time. This result shows that Yoshixolis related to physical property and function property of substance (forexample, actin such as contraction proteins and hydrolysis reaction ofATP as energy source) which is concerned with a flagellum movement ofspermatozoa, so that Yoshixol is related greatly on a movement andsignal transduction of the procaryotes and eucaryotes, and on thedynamic behavior which is essential qualities of living organism.Moreover, from the knowledge that these movements of cells are involvedin microfilaments and microtubles which is constricted from the proteinsassembly, a morphological change of this spermatozoa due to treatmentwith Yoshixol was investigated by transmission type (JEM1200, EXII,JEOL, Ltd.) and scanning type (JSM-6000F, JEOL, Ltd.) electronmicroscopy. The outside of normal flagellum with regular basic structureof 9+2 is enclosed with a cell membrane and, there was the axialfilament which structure is related to a movement is observed inside.The axial filament has two pairs of tubles (centrum pair) that existmainly on the center and nine double tubles that exist in a periphery(circumscription canaliculus). The surface structure contributed to themovement was observed to make ring formation likely to the doughnuts,which are configured orderly and smoothly on the surface. But, thoughmorphological aspect as a whole of spermatozoa was not altered-by thetreatment with Yoshixol, many particles with a size of 10-30 nm on thesurface were observed likely to be blowed out, when the surfacestructure of flagellum was investigated by a magnification. And also,ring formation likely to a doughnut in which-region is contributed tothe movement was not found and, adhesion of small particles werenoticeable (referred FIG. 28). Moreover, while fundamental fiber unitsof a flagellum were maintained on the transmission electron microscopicobservations, there were a lack of continuity of the membrane whichsurrounds fibers of the surface and a lack of regular alignmentconfiguration whose fiber units (myofibrille) inside of the each unit offiber construction. And, an appearance of high-density aggregatedsubstance was found (referred FIG. 29). Moreover, the morphologicchanges in the surface and intracellular organella of the head were notfound in contrast to findings of marked changes in flagellum. Theseresults show that in the present situation which many interests involvein a role as cytoskeleton which is related to dimer formation of actinand tubulin (for example, oncogeneis, metastasis, cell death and so on),Yoshixol can apply into inhibitory agents of bacteria prolifelation forprocaryotes, antibacterial agents and/or anticancer agents foreucaryotes as well as application as the contraceptive agents which cancontrol and/or inhibit a motility of spermatozoa. Moreover, it is shownthat Yoshixol can apply into inhibitory agents or control agents foregenerating function which is based on the polymerization reactionrelated with morphogeneis, cell adhesion and each life events (forexample, immune response).

[0784] <Effect on Changing a Physical Property with Macromolecule.>

[0785] Changes in physical properties (for example, change of glossy orshiny and luster, accurate boundary on casting formation, smoothness andhomogeneity of surface, transparence, texture minuteness, change inquantity and so on) of macromolecules due to Yoshixol were investigated.In other words, 100 μl of Yoshixol per 100 g of following each substancewas added. Then, each sample was processed with heating within a watertank until the melting followed that the melted sample was poured into afilling teeth-marks phantom of caries which is used at theodontotherapy. After cooling and taking out from a template, in thestate which became solid, the surface of each sample was observed by 2-5times magnification with loupe. A fall of melting point in the allsubstances treated with Yoshixol, which substances are shown below, wasfound in comparison with the object which is not added. In octadecanol(Wakou Jyunyaku Ltd., Osaka) with Yoshixol, glossy, shiny and lusterbecame better and boundary also became more clear and sharp. In stearicacid (Wakou Jyunyaku Ltd., Osaka) with Yoshixol, an appearance oftransparence, smooth of a surface and texture minuteness ischaracteristic. In lauric acid (Wakou Jyunyaku Ltd., Osaka) withYoshixol, smoothness and transparence appeared. In dodecanol (laurylalcohol) (Wakou Jyunyaku Ltd., Osaka) with Yoshixol, melting becamemarkedly and casting form could not be kept by room temperature. Inpalmitic acid (Wakou Jyunyaku Ltd., Osaka) with Yoshixol, a soft feelingappeared. In myristic acid (Wakou Jyunyaku Ltd., Osaka) with Yoshixol,clearness of boundary and homogeneity appeared, and also in tetradecanol(miristyl alcohol) (Wakou Jyunyaku Ltd., Osaka) with Yoshixol, clearnessof boundary and homogeneity appeared. In hexadecanol (Wakou JyunyakuLtd., Osaka) with Yoshixol, it was a characteristic that textureminuteness and transparence fell. In decanoic acid (Wakou Jyunyaku Ltd.,Osaka) with Yoshixol, a rough surface and a small prominence appearedthough luster and boundary clearness appeared. In polyethylene glycol1000 (Wakou Jyunyaku Ltd., Osaka) with Yoshixol, clearness of boundaryand smoothness get worse. In polyethylene glycol 1540 (Wakou JyunyakuLtd., Osaka) with Yoshixol, transparence, smoothness and homogeneitygets better. In polyethylene glycol 2000 (Wakou Jyunyaku Ltd., Osaka),polyethylene glycol 4000 (Wakou Jyunyaku Ltd., Osaka) and polyethyleneglycol 6000 (Wakou Jyunyaku Ltd., Osaka), an increment effect of textureminuteness, transparence and expansibility was found after Yoshixol. Inaddition, luster, clearness of boundary, homogeneity of a surface,transparence and texture minuteness were found in N-isopropylacrylamide(Aldrich Co. Milwaukee, Wis., USA with Yoshixol. Moreover, in order toinvestigate an effect of Yoshixol on polymers as macromolecules,acrylate polymers were tested as one of a concrete example. Standardgrade of lauryl methacrylate 471, methyl methacrylate 48, ethylmethacrylate 126, isobutyl methacrylate 140 and butyl methacrylate 320(polymer kit, acrylate polymer standard 18336-9, Aldrich Co. Milwaukee,Wis., USA) were used and were observed at room temperature. When 150 μlof Yoshixol was added in 1 g of each acrylate macromolecules, allsubstances becomes liquid and glass-like transparent and, powdered andcrystal configuration disappeared so that these were changed in thehomogeneous substances. In addition, when 100 μl of Yoshixol is addendumin the above lauryl methacrylate 471, fluidability increasedimmediately. Floating viscidity appeared after 2 weeks and, there wasseparation of solid component with translucent and fluidable componentone month after adding Yoshixol although the volume of sample wasdecreased in the group without Yoshixol. In methyl methacrylate 48, adried powder state disappeared immediately after addendum of Yoshixoland, fluidability increased and was likely to a rice cake so that itbecame paste-like with after 2 weeks and adhered on the wall of tube,and volume of this sample was increased after 1 month. Dried powder-likeaspect disappeared even in ethyl methacrylate 126 immediately afteraddendum of Yoshixol and, viscidity with lumpy appeared-immediatelyafter addendum of Yoshixol so that after 2 weeks it became paste-likeand it adhered in the wall of tube. More transparence was increasedafter 1 month. Dried powder-like aspect disappeared even in isobutylmethacrylate 140 and, viscidity with lumpy transparence appeared so thatviscosity was increased and it became paste-like after 2 weeks. Thoughthe sample which adhered on the wall of tube was transparent, anunreaction part of substratum had a color in a powdered state beforetreatment with Yoshixol. In butyl methacrylate 320, a powdered statedisappeared and viscidity, lumpy and transparence were increased afteraddendum of Yoshixol. The sample was adhered paste-like on the wall oftube. Though there is a difference of transparence according to theadhesive state after 2 weeks, a transparent part of the sample had avitrified transparence. So, the sample became to be less viscidity andmore homogeneous glass-like mass with transparence after 1 month, andthe quantity of the sample also was increased. In addition, changes inthe physical property of other polymers in acrylate group wereinvestigated by using standard grade polymers (polymer kit, polyacrylatestandard 18338-5, Aldrich Co. Wis., Milwaukee, USA). The kit containedpoly(2-ethylhexyl acrylate), poly (methylacrylate), poly (octadecylacrylate), poly (ethyl acrylate) and poly (butyl acrylate). Then, 500 mgof each sample was treated with 200 μl of Yoshixol at room temperature.An increase in fluidability occurred in poly(2-ethylhexyl acrylate)immediately after treatment with Yoshixol, however, color of the sampledid not change. Fluidability and capacity were increased more after 2weeks, and also the refraction of light was changed. In addition,fluidability was increased after 1 month in addition, and a capacityalso was increased by twice. In poly (methylacrylate) with Yoshixol, anincrease in fluidability and a cubic capacity was observed, and opticaltransparence also became better. Fluidability has been enhanced after 1month, and a capacity also did a gain almost 2-3 times. Inpoly(octadecyl acrylate) with Yoshixol, a dried powder statedisappeared, and the sample became homogeneous and lumpy mass. In poly(ethyl acrylate) with Yoshixol, fluidability was increased markedly andbecame fluidable, and a marked increase in capacity occurred so thatfluidability of the sample was increased and volume of the sample wasgained by 3 times after 1 month. In poly (butyl acrylate) with Yoshixol,fluidability also was increased. In addition, the fluidability of thesample was increased more after 2 weeks and the sample became to be morefluidable. A volume of the sample was increased by almost 2-3 times aswell as an increment of fluidability after 1 month. Moreover, changes inthe physical property of other polymers were investigated by usingstandard grade polymers (polymer kit 18337-7, Aldrich Co. Wis.,Milwaukee, USA). The-kit contained poly(dimethyl siloxan), poly (vinylacetate), poly (methyl methacrylate), poly (vinyl chloride) andpolycarbonate resin. Then, 500 mg of each sample was treated with 200 μlof Yoshixol at room temperature. In poly(dimethyl siloxan) withYoshixol, though Yoshixol was difficult to be mixed with the sample justafter the treatment and it was on the top as a liquid layer, an increasein a cubic capacity and fluidability occurred after 2 weeks. A viscosityand a quantity of the sample were gained after 1 month, however, opticaltransmission was decreased. In poly (vinyl acetate) with Yoshixol,viscidity was increased and the sample was adhered on the wall of tubethough a fluid component was observed on the bottom of the tube.However, fluid component in the tube disappeared after 2 weeks so thatthe sample became to be a viscous solution with transparence and anincrement of transparence was observed. In addition, transparence of thesample became very stable after 1 month. In poly (methyl methacrylate)with Yoshixol, the sample was frosted glass-like and crystal after 1month though it resulted in the state which was massive homogeneouslywith transparence immediately after Yoshixol. In poly (vinyl chloride)with Yoshixol, a dried powder state of the control sample disappearedand the sample became to be an ununiformed mass with small granules. Amarked change was not observed when the sample was placed at roomtemperature. In polycarbonate resin with Yoshixol; a powder-like granuledisappeared immediately after Yoshixol and the sample became to beadhesive. Additionally, though transparence fell after 2 weeks and areflected light was not observed by a frosted glass-like change, avolume of the sample was observed after 1 month. Moreover, when 100 μlof Yoshixol are added to 200 mg of N-isopropylacrylamide (Aldrich Co.Milwaukee, Wis., USA), Yoshixol was permeated into a crystal as likelyas that a sugar indulges, in water. Subsequently, after 2-3 minutes, aformation of substance with transparence occurred from a side of thebottom of the tube without generation of fever and vapor resulting in asherbet-like substance after 4 hours. And, the sample after 2 weeks wasfrosted glass-like with less transparent.

[0786] Moreover, 100 μl of Yoshixol was added in 200 mg of polyethyleneglycol phenylether acrylate (Aldrich Co. Milwaukee, Wis., USA),polyethylene 125,000 (Aldrich Co. Milwaukee, Wis., USA) and polyethylenelow density (Aldrich Co. Milwaukee, Wis., USA) as another macromoleculesin polyethylene group. Each sample was observed at room temperature. Inpolyethylene glycol phenylether acrylate with Yoshixol, an increase influidability was observed just after the treatment. As a time passed, itwas also observed increases in optical transparence and volume of thesample. Moreover, in polyethylene 125,000 with treatment, an adhesionbetween granules occurred so that each granule of the sample became tobe adhered after 2 weeks though a grained form has been left. Inaddition, in polyethylene low density with the treatment, the samplebecame to be bigger granular from powder-like. Moreover, in order toinvestigate an effect of Yoshixol (100 μl) on macromolecules inpolystyrene group, 200 mg of polystyrene 45,000 (Aldrich Co. Milwaukee,Wis., USA), polystyrene 280,000 (Aldrich Co. Milwaukee, Wis., USA) andpolystyrene standard (Aldrich Co. Milwaukee, Wis., USA) were used. WhenYoshixol are added on polystyrene 45,000, powder-like granules ofpolystyrene 45,000 disappeared, and viscidity of the sample appeared,and the sample became transparent and a crystal structure of the samplewas lost. These properties did not alter even after 1 month. Powder-likegranules disappeared in polystyrene 280,000 after treatment so thatparticle configuration of the sample was lost in parallel with anappearance of viscidity. Optical transparence became to be better likelyas a transparent glass even when 1 month has been passed. A similarchange in physical property was observed in polystyrene standard.Moreover, when 100 μl of Yoshixol was added in 200 mg of hydroxylatedpolyethylene vinyl alcohol (Aldrich Co. Milwaukee, Wis., USA), thesample became lumpy with ununiform and easy breakage from driedpowder-like substance. When the time was passed, the sample became driedpowder-like lumpy again, and also became adhesive to the wall of tube.These results show that Yoshixol can improve the physical property ofmacromolecules and the function which is generated or induced bystructure of macromolecules.

[0787] Moreover, since investigations above-mentioned were mainlycarried by macroscopic observations, the microscopic observations weredone to investigate effects on a change in physical property of eachmacromolecules. Changes in physical properties of macromolecules weremeasured by a digital scanning calorimeter (DSC-50, Shimadzu SeisakushoLtd.). Data from the digital scanning calorimeter is displayed as acurve which is converted a signal of temperature deviation (ΔT) fromstandard substance (at present measurement, alumina was used) against atime or a sample temperature so that area of the part which was enclosedbetween a base line and a peak is proportion to a thermal energy whichis needed for a fusion of sample. Thus, since the thermal energy whichwas supplied to the sample at a constant pressure is identical with aincreased amount of enthalpy in the sample, decrement effect of enthalpyof sample (decrement of heat capacity at constant volume andcondensation rate) is displayed as a peak of falling downward on aphenomenon of changing physical property which is accompanying with adiscontinuous change of the enthalpy against temperature such as theprimary phase transition of a crystal and a fusion of sample. Therefore,peak area is regarded as a saltation quantity of enthalpy. Any change ina heat capacity measured by digital scanning calorimeter did not observein stearic acid and lauric acid between before and after treatment.Though a slight fall of melting point was investigated in myristic acidand palmitic acid (100 μl of Yoshixol per each 100 g, referred FIG. 30),a large change in heat capacity was not found. On the other hand, andecrease in enthalpy between 20 and 60° C. on polyethylene glycol 1000was disappeared after Yoshixol so that a phase which thermal capacitybetween 120 and 160° C. became a decrement reaction of enthalpy wasfound (referred FIG. 31). In polyethylene glycol 4000 with Yoshixol, afall of melting point was observed. When 100 μl of Yoshixol was added in200 mg of polystyrene 280,000, a phase of a decrement reaction ofenthalpy around 30° C. and 280° C. was appeared (referred FIG. 32). When200 μl of Yoshixol was added to 500 mg of methyl methacrylate, adecrement reaction of enthalpy between 230° C. and 340° C. was appearedthough melting point did not change. Moreover, when 200 μl of Yoshixolwas added on 500 mg of ethyl methacrylate, a decreased and increasedreaction of enthalpy was inhibited as the whole (referred FIG. 33). Evenwhen 200 μl of Yoshixol were added on 500 mg of isobutyl methacrylate,two peaks on an increase reaction of enthalpy between 60° C. and 250° Cwere appeared newly and, an inhibition of maximal increase in enthalpyaround 320° C. was found. In addition, a phase transition phenomenon wasobserved in macromolecules in acrylate group such as lauryl methacrylateand poly (methylacrylate) by treatment with Yoshixol. In 500 mg of poly(vinyl chloride) treated with 200 μl of Yoshixol, a decrement reactionof enthalpy around 300° C.-380° C. became to be about 2 times incomparison with the control (referred FIG. 34). When 100 μl of Yoshixolwas added to 100 g of polyethylene glycol 4000, a new peak which showsan increase reaction of enthalpy between around 44° C. and 50° C. wasfound. When 200 μl of Yoshixol was added to 500 mg of poly(methylacrylate), an increase reaction of enthalpy in a range between60° C. and 360° C. was inhibited (referred FIG. 35).

[0788] Moreover, when expansibility of poly (vinyl chloride) wasobserved by a heat machinery analysis equipment (TMA-50, ShimadzuSeisakusho Ltd.), an increased reaction of volume in the control samplewas found around 315° C., however, an increased reaction of volume in500 mg of poly (vinyl chloride) treated with 200 μl of Yoshixol wasdisappeared and a decrease in a condensation rate was found (referredFIG. 36). These results show that Yoshixol has a capacity which canimprove a physical property with molecules and macromolecules, namely athermodynamic property (for example, energy storage capacitance andinternal energy state, change of structure due to change in entropy).And also, Yoshixol can improve a functional property which is induced orgenerated by structure of molecule and macromolecules.

[0789] <Effect on Changes in Molecular Weight of a New Synthesized Dimerwith Seven Base Pair>

[0790] DNA or RNA synthesis device (392-25 type, Perkin-Elmer Co.) wasused and 7 base alignment (CTTCGGA) and (CTTCGGG) new synthesis dimer(5′>CTTCGGACTTCGGA<3′) and (5′>CTTCGGGCTTCGGG<3′) were synthesized.Then, an effect of Yoshixol on a change in molecular weight of the dimerwas investigated. This pellet was dissolved on 50 μl of tris EDTA, andOD260 was measurement by 100 times attenuation so that concentration wasturned into equality (5 ng/μl) by tris EDTA and distilled water. And, 4μl of an adjusted synthesis dimer was labeled at 5′-terminal end of thedimer with 4 μl of ATP which was labeled by P32. In addition, afterprocessing the dimer with 1 μl of polynucleokinase (TaKaRa, Tokyo) for30 minutes by 37° C., the solution was heated at 70 ° C. for 5 minutes.Afterward, 65 μl of tris EDTA, 1 μl of glycogen and 190 μl of chilledethanol were added and were mixed. And, it was centrifuged over 10minute by 16,000 cpm. After taking the supernatant out, the pellet wasmade dry. Again, it was dissolved by 50 μl of tris EDTA and, 1 μl of thesolution with radioactivity was mixed with urea (15 g), acrylamide (5.7g), bisacrylamide (0.3 g), tris boric acid EDTA (3 ml), 10%ammoniumpersulfate (0.1 ml) and N, N, N, N-tetramethyldiamine (15 μl) todistilled water, so that the volume was made to 30 ml in total. Then,20% gels were made and the electrophoresis with constant voltage of 10watt was performed to be exposed on a film. Changes in molecular weightwith the dimers were investigated by the sample which was consisted of 2μl of the solution which was dissolved by final tris EDTA-with 2 μl ofYoshixol. As the control sample, 2 μl of distilled water was added tothe solution. Then, each test sample was given 6 μl of the stopsolution. Change in molecular weight of the synthesized dimers withYoshixol did not differ from that without the treatment (referred FIG.37). Therefore, this result shows that Yoshixol does not change adistribution of molecular weights with new synthesized dimers(5′>CTTCGGACTTCGGA<3′) and (5′>CTTCGGGCTTCGGG<3′) and does not change atleast a primary structure.

[0791] <PCR Effect on DNA Template of a New Synthesis Dimer with BasePair>

[0792] Effect of Yoshixol on PCR was investigated by DNA template whichwas extracted from snake (blue-green snake, captured at Matsumoto city,Nagano). The new synthesized dimer of (5′>CTTCGGGCTTCGGG<3′) with 7base-pair alignment (CTTCGGG) above-mentioned was used as a primer. PCRreaction was done by use of DNA thermal cycler (PJ-2000) made in PERKINELMER CETUS company.- The following six combinations were prepared forthe test samples. Those are two kinds of samples which consist of 5 μlof primer (100 pico mole/μl) with 5 μl of Yoshixol (P+) and withoutYoshixol (P−). In addition, two kinds of samples which consist of 5 μlof snake DNA (500 ng/μl) with 5 μl of Yoshixol (D+) and without Yoshixol(D−). And, additional two kinds of samples which consist of 1 μl ofpolymerase enzymes (Recombinant Taq DNA Polymerase, No. R001A, TaKaRaShuzo Co., Otsu city: 5 unit/μl) with 1 μl of Yoshixol (Pm+) and withoutYoshixol (Pm−). After each sample was placed for 10 minutes at roomtemperature, each sample was diluted in distilled water. And, it isadjusted in a primer solution of 10 picomole/μl, DNA solution of 50ng/μl and a polymerase enzymes solution of 0.5 unit/μl. Then, thefollowing combinations were prepared. On PCR, a primer solution of 5 mlwhich is diluted mentioned above, 5 ml of DNA solution, 5 μl of buffersolution for PCR reaction, 0.25 μl of polymerase enzymes solution and 4μl of dNTP mixed solution were added in distilled water to be made totalvolume of 50 μl. Combination of each sample is following five groups.First, each sample is not added Yoshixol as the control (P−, D−, Pm−).Second is the sample which only a primer has processed by Yoshixol (P+,D−, Pm−). Third is the sample which only DNA has processed by Yoshixol(P−, D+, Pm−). Fourth is the sample which polymerase enzymes alone hasprocessed by Yoshixol (P−, D−, Pm+). In addition, fifth is the samplewhich concentration of Yoshixol for the polymerase is increased to 100times on P−, D−, Pm+series above mentioned (P−, D−, Pm+A). In eachcombination, amount of cDNA synthesis was amplified by a PCR method andwas measured. On the group of P−, D−, Pm− which all samples were nottreated, 4 bounds between a molecular weight of 0.5 and 1.2 kb werefound. Also, the bounds in P−, D−, Pm− did not differ from those in P+,D−, Pm− and P−, D+, Pm−. But, on the group of P−, D−, Pm+, only onebound at lowest molecular weight within 4 bounds was appeared. Inaddition, any kind of bounds did not observe on the group of P−, D−,Pm+A (referred FIG. 38). This result shows that Yoshixol controls orinhibits functional generation of polymerase enzymes which is related totranscription and/or amplification of the base-pair alignment generatedby DNA template which consists of many base-pair alignments. It is to beneedless to say that inhibitory effects of molecular generating and/orinducing functions which was carried in claims 1-11 in this inventionare not restricted by the primer which is new synthesized dimer(5′>CTTCGGGCTTCGGG<3′), snake DNA and polymerase enzymes demonstratedhere.

[0793] <Effect of Yoshixol on a Change and a Modulation in Absorbance ofWavelength of Molecule with Pigmentums>

[0794] In order to investigate an effect of Yoshixol on a change and amodulation of wavelength of molecular of pigmentums,eosin-5-iodoacetamide (Molecular Probes Inc., USA), evans blue (WakouJyunyaku Ltd., Osaka) and ethidium bromide (Molecular Probes Inc., USA)was used. After Yoshixol (10 μl) was added to 1 ml ofeosin-5-iodoacetamide solution (10 mg/l ml), 1 ml of evans blue solution(1 mol) and 1 ml of ethidium bromide solution (10 mg/ml), the absorbancewas measured by a spectrophotometer (BIO SPECTRO, Beckman Co. USA). Thefundamental wave length band which each pigmentums did not change withor without adding Yoshixol. And, though a quantitative and qualitativechanges also did not found as well as the fundamental peak wavelength, awave length band below 260 nm showed a great change. Especially, colorof ethidium bromide with Yoshixol was observed to become a lack oftransparence from a transparent dark and red. Such color after thetreatment is observed by a naked eyes as almost a white and pink justlike a ripe peach. In this case, major difference was foundquantitatively and qualitatively in a wave length band between 270 and200 nm which was measured by a spectrophotometer (referred FIG. 39).This result shows that Yoshixol can modulate a wave length band ofpigmentums.

[0795] <Effect on Surface-Active Agents and/or Surfactants>

[0796] Moreover, effects of Yoshixol (50 μl) on surface-active agentsand/or surfactants were investigated by use of 20 ml of each detergentfor kitchen use commercially (for example, CHERMING, Lion Co.: NATERA,Lion Co.: MOA, Kao Co.), which consist mainly of alkyl ether sulfateester sodium, fatty acid alkanolamido and polyoxyethylene alkyl ether.And, effects of Yoshixol (50 μl) on shampoos were investigated by use of20 ml of each shampoo for hair washing use commercially (for example,PANTEN, Maxfacter Co.: LAX STYLING, Japan Riever Co.: ESSENTIAL STYLING,Kao Co.), which consist mainly of lauryl sulphate, paraven, cetylalcohol, edetic acid, propylene glycol, polyoxyethylene laurylethersulphate. Each detergent and shampoo treated with Yoihixol became betterfoamed, better bubbled with sensitive texture, less adhesive and morebright colored, and it can wash out easily a soil of oiliness with aless amount of water. In addition, though a large difference on anaspect of each detergent and a shampoo which is added Yoshixol did notfind, the viscosity of each detergent and a shampoo with the treatmentdecreased in the comparison with the non-treated one measured at 30° Cby a viscosimeter (Vismetron VEA-L, Shibaura System Co.)(referred Table1). Moreover, a relationship of slip velocity-slip stress also decreasedafter the treatment. This result shows that an adding process ofYoshixol on a detergent and a shampoo which is already marketed canimprove surface active effect and it's property with a detergent and ashampoo. TABLE 1 Change in Viscosity (CP) of Each Detergent Before andAfter Treatment with Yoshixol MORE CHARMING NATERA Before 66.9 62.2 70.2After 62.9 53.3 63.5

[0797] <Effect on Each Fatty Acid>

[0798] By adding 5 g of lauric acid (Wakou Jyunyaku Co., Osaka), 5 g ofmyristic acid (Wakou Jyunyaku Co., Osaka), 5 g of palmitic acid (WakouJyunyaku Co., Osaka), 1 g of linolic acid (Wakou Jyunyaku Co., Osaka), 5g of stearic acid (Wakou Jyunyaku Co., Osaka) and 1 g of oleic acid(Wakou Jyunyaku Co., Osaka) into 50 ml of sodium hydroxide solution (1N), a soapy substance was made (neutralization method). Then, the effectin the event that Yoshixol was added and investigated. A soapy substancewith 50 μl of Yoshixol showed a property of better foamed, scarced,lavaged and less adhesive in comparison with a soapy substance withoutYoshixol. Even though it was placed freely in a room over 6 months, abrown change did not occur in comparison with a soapy substance withoutYoshixol. This result shows that Yoshixol is useful as antioxidants fora soap which is made from fatty acids, vegetable oil or animal oil, andthat Yoshixol can improve and/or make better a property of soaps whichis planed and manufactured freely.

[0799] <Concerning Acute and Chronic Toxicity>

[0800] In order to investigate a toxicity in vivo, the solution whichwas mixed 50 μl/Kg of Yoshixol with 1 ml of 20% glucose solution wasadministered intravenously in unanesthetized animals (rabbit and dog).After intravenous injection, transitional increase in respiration rate,increase in blood pressure and heart rate and active movements of anextremity (not convulsion) were observed for 1-2 minutes after theadministration. Although an increases in a respiration rate and bloodpressure remained during the observation period of 2 hours, an abnormalbehavior was not found. On examination of blood, hyperchromic anemia atthe maximum level occurred 3 days after administration followed by arecovery to the normal after 1 week. A change in platelets was notobserved and, white blood cells increased 3 days after administrationfollowed by a recovery to normal level at 1 week after administration.Though these animals were observed over 1 month, any abnormal behaviordid not found. Also, after they were sucrified by intravenous injectionof potassium chloride solution under deep anesthesia after 1 month, anypathological findings were not observed macroscopically andmicroscopically in the vital organs. This result shows that effect ofYoshixol is low toxic in vivo, and a side effect is less. Even thoughintravenous administration alone was done, it may be confirmed that itis safety.

[0801] Moreover, effects of chemical substance(4,4-dimethyl-2-cyclohexen-1-one) that all of substituent R1, R2, R3,R4, R5, R6 shown in general formula (1-b) and all of substituent R3, R4,R5, R6 shown in general formula (3-b) is hydrogen were investigated onall of parameters which were demonstrated by Yoshixol above-mentioned inthis invention. As a result, this substance also provided to be able tocontrol, inhibit and/or block function which is generated bymulti-dimensional structure similarly to Yoshixol mentioned above. Inaddition, higher dosage was needed to be obtained qualitatively anidentical effect to the above-mentioned effect of Yoshixol. Then, theconcentration of 4,4-dimethyl-2-cyclohexen-1-one was required about30-100 times dosage of Yoshixol on the biological samples, and about10-50 times dosage of Yoshixol on lower molecular substance andmacromolecular substance of non-living samples.

[0802] <Summary of Primary Effect and Mechanism, and its Significance>

[0803] Although it was demonstrated effects of Yoshixol as arepresentative compound in this invention, this invention is notrestricted mentioned above by the demonstrating experiments which wasshown here. This invention demonstrated a wide proofed effects andefficacies from a molecular level to the over all organism. To cite eachreference about each scientific back-ground is far from the aim of thisapplication so that the following two issues are cited as references ofscientifically known events.

[0804] <ref. 1>by Bern and Levy, Physiology, Sanders Publishing Inc.:

[0805] <ref. 2>by Alberts, Ray, Lewis, Raff, Roberts and Watson,

[0806] The Molecular Biology of the CELL, Garland Publishing Inc.:

[0807] As significance of this invention, it is the first time toprovide possibilities with concrete examples to modulate a reactionprocess in molecular level and a function generated or induced bymulti-dimensional structure which is produced by molecular-composedmacromolecules. And, it is also the first time by concrete examples toprovide possibilities to change function and/or block biologicalfunction witch is induced or generated by multi-dimensional structurewhich is constricted from macromolecules substances. Moreover, thesignificance in this invention is so great because that the providedcompounds in this invention can inhibit and/or block function which isinduced or generated by the multi-dimensional structure which hadspecies difference of the cell membrane that is determined accordingeach species evolutionally and is constructed for coexistence with theexternal world. And, the significance on scientific history is alsogreat because it is clearly discussed that effects and mechanism of thecompounds in this invention can understand by the theory of molecularorbital dynamics. In addition, the practical significance emphasized inthis detailed description of this invention. The social significance inthis invention is not only effects of the compounds, but also to beexpected a necessary effect by use of the known mathematical simulation(for example, approximation of lone electron pair) concerning whetherthe compound is useful to human being or not, because that the compoundsprovided in this invention has extremely simple chemical structure. Itis to be able to forecast sufficiently from demonstrating experiments inthis invention and known scientific facts of molecular biology that forexample, the effectiveness on the virus which is the filterablepathogenic microbacteria that is made up of macromolecules, namely onHIV infectious disease which is a world-wide problem at present time.Moreover, this invention has some suggestive ways coexistence between ahuman being including an environment on the earth and the nature as wellas forecasting an interaction of drugs and an onset of side effects withcombined use of drugs, and an early forecast of an appearance of theresistant strain and it's preventive step that is considered ecologicalsystem. The significance of this invention was darely carried because ofeternal happiness of a human society and uncontroversial coexistence.

[0808] The brief comments of the logical explanation which is regardedas necessity to understood from claims 1 to claims 46 in this inventionis carried following with both common mechanism as demonstrated inthis-invention, with distinguishing effects on living organism andsubstances as an inanimate object. However, it is needless to say thatthis invention is restricted by this description about the significanceand mechanism. Thus, it is possible to explain effects of this inventionintegrately by interpreting mechanism of this invention on quantumtheory of molecular orbital dynamics and thermodynamics. Then, it iswidely known that each molecule has configuration, conformation andmolecular orbital and, there is a space region corresponding to electrondistribution. By an energy state on basis of molecule, it is possible tobe explained the configuration of a molecule itself, physio-chemistryproperty and, interaction and a reaction rate of combining withdistinctive molecule by the wave equation and the frontier theory ofmolecular orbitals. (bibliography: Yuki Denshi Ronn Kaisetu, 4th ed, byMinoru Imoto, Tokyo Kagaku Doujinn,1990; Introduction of frontierorbitals, by Fleming, supervised by Kenichi-Fukui, translated by TomodaTakeuchi., Kodansha, 1992; How understand molecular orbital, 2nd ed, byMasayuki Yosida; Tokyo Kagaku Doujinn, 1992). And, a theoreticalexplanation of many chemical reactions can have been done by based ontheory of organic electron, theory of molecular orbitals and quantumtheory in organic chemistry for each molecule. For example, a rule ofWoodward-Hoffman is also the one example. Generally, as it is away fromatomic nucleus, existential density of electron changes and, a distanceequivalent to the highest peak is a location that electron exists mostabundantly (equilibration distance). Moreover, existential probabilitiesin an electron cloud which is in the location where generally electroncan expand is determined following energy. It is the logical conceptwhich this has systematized as quantum theory. On binding with of C andH (covalent bond) as one example of orbital with hybridization, if H andC can be overlapped, two electrons are coupled on both C and H. When twoelectrons turns a spin into reverse so that one bond is formed theinternal energy which an atom itself has gets lower and stabilization inorder to release an enormous amount of the overlapping energy. Thus,binding energy is generated. In contrast, in order to make an originalatom by splitting C—H bond, this binding energy must be added newly bysome processes. Moreover, molecule has orbitals which is quantumized(There are constant orbital energy with discontinuity) between unstableorbitals and stable orbitals. Thus, it is known that a pair of twoelectrons enters into the orbital with a reversed spinfrom a stableorbital in order. With regard to an overlap of molecular orbitals, thereis (+) and (−) phase so that molecules which have the same coincidenceof phase only can be piled each other up, resulting in thestabilization. In contrast, if there is a phase difference as (+) and(−), it is also known that each molecule can not overlap so that eachmolecule is repulsed resulting in instability. Such matters is a basictheory of molecular orbitals. Moreover, though hydrogen ion is inscribedas H⁺, H⁺ is proton itself. Thus, elementary particle can not be able toexist singly in a container such as a beaker and it is very instable.Though this point is also ultimate knowledge in the science, there iseven the important matters-which is easy to be forgotten unexpectedlywhen life events is understood. Thus, an equilibration relation of“H₃O”⁺ with H₂O are kept certainly in the place where water exists. Thisis important matter to need remembering when function is considered. Inconsideration of such theory of charge-transfer and molecular orbitals,it is extremely reasonable to grope a possibility which has at potencyof control, inhibition and/or blocking of functional property andmorphologic structure with functional macromolecules and livingorganism, so that this point consists of a part of logical basisconcerning inhibitory effects of molecular generating and/or inducingfunctions, which was carried in claims 1-11 of this invention.

[0809] Moreover, on generation of a combination in binding molecularorbitals, each s orbital was overlapped to become stable a bind and,each sp orbital was overlapped on the same directional axis to become abind and, p orbital was overlapped to becomes bind when it stoodopposite to each other on the same directional axis. In addition, ongeneration of n bond, p orbital becomes n bond when p orbital stood in aline in a parallel lengthwise. When it can not be matched, s orbital cannot bond even if it is overlapped to p orbital with a different axis (inother words, atomic quadrupole moment). In addition, in regard to phase,p orbital on an identical x axis becomes a bond and, p orbital on pyorbital or px orbital become to be in parallel, resulting in n bond.Since a direction of p orbital differs from py orbital and px orbital onright angle, the overlap does not occur. And, the binding does not occurwhen the phase differs between each molecule because of anti-bondingmolecular orbital. In addition, electron isomerising effect (E effect)becomes in n bond with the double bond so that it differs greatly fromthat I effect is n bond. Because O group is the 6th group, if O grouphas six electrons which belongs to O itself, O group does not have anability of proton discharging and electrically is neutral. However, forexample, when O group has 7 electrons, electric charge on negative isnaturally. This is fundamental and characteristic event of the carbonylgroup which inhibitory or blocking agents of molecular generating and/orinducing functions which is carried in claims 1-11 of this invention.Moreover, delocalization of n electron and delocalization energy arealso important. When n electron is distributed, the molecule becomesstable so that only amount of energy which became stable results indelocalization energy of electron. Carboxyl group, —C (═O)—OH, has theproperty or configuration that gives H⁺ to other molecule. As a secondreason which is easy to discharge H⁺, an anion which is —CO—O— afterwhen H⁺ has been produced is distributed so that delocalization energyor resonance energy is generated. By discharging H⁺, it can bestabilization still more. Thus, this state becomes to definitivelyreproduce the first factor that can release H⁺. But, a formula ofH₃O⁺×OH⁻=constant is usually made up of every aqueous solution includingliving organism. Such released proton is utilized as an internal energyfor disordering in living organism with thermodynamic non-equilibrationand opened system. The proton is utilized as ordering or stabilizingenergy in proton receivable substances with thermodynamic equilibrationand closed system. In order to inhibit or block each function (includingmolecule recognition) generated by multi-dimensional structure withoutchanging the primary structure, it is ideal that the compound has aproperty of both electrophilic and nucleophilic nature and, the compoundis neutral substance which has not a potency of releasing proton. On areaction orσ−Π interaction on Π electron group, theory of frontierorbitals is an important concept that a reaction is definitive betweeninteraction of HOMO molecular orbital and LUMO molecular orbital. Forexample, since double bond is formed from both σ and Π bonds, a reactionis generated in the part which electron density is large. When“excitation” of carbonyl group is turned into an example, electron pairof Π covalent bond which links between C and O by double bond is basedon E effect and has a possibility to pull toward O . An addition ofcarbonyl group is called nucleophilic addition reaction. A property with“excitation ” of carbonyl group is that oxygen takes electron so thatmore negative charges are easily increased. Though C═O has n bond,bonding molecular orbital with electron affects to anti-bondingmolecular orbital of C═O group because that an anion has excessiveelectrons on a molecular orbital method. Thus, HOMO molecular orbital ofan anion substance and LUMO molecular orbital of C═O result in aperturbation state. From this point of view, a part which a compound iseasy to react depends on a magnitude of coefficient C of HOMO molecularorbital or LUMO molecular orbital and symmetry of phase with constitutedatom orbital. In addition, an importance factor which dominates anactivation energy of a chemical reaction is an electrical force on thebasis of organic chemistry and electron theory. Thus, a polarization orelectron transferring must occur in a reaction with neutral molecule sothat it becomes important whether electron density in the reactioncenter is higher or lower. A substance concerned with morphologicformation and function of living organism produces a generation offunction and a differentiation of function due to molecule recognitionor in the region of reaction center by changing electron density due toconformations. In the frontier orbitals which is one of concepts that amagnitude of the activation energy which shows hardness of such areaction is determined by the energy which is required to be localized nelectron localization in a transition state, the position that occurselectrophilic reaction, nucleophilic reaction and radical reactionwithin one molecule is determined by the following. An electrophilicreaction at a basal state occurs in a position with highest density oftwo electrons which belongs to highest occupied molecular orbital (HOMO)and, a nucleophilic reaction occurs in the position of highest densitywhen two electrons are stationed on lowest unoccupied molecular orbital(LUMO) at a basal state. A radical reaction occurs in the position whichis largest sum of two electron densities when each electron is stationedon each HOMO and LUMO. In this way, the important factor whichdetermines a chemical reaction is that as a condition of morestabilizing a reaction, it is needed to be consistent with symmetrybetween HOMO of an electron donative substance and LUMO of an electronacceptable substance. Thus, stabilization energy in the system isobtained only when symmetry between HOMO and LUMO is with thecoincidence so that the chemical reaction becomes easy to be generated.And also, when a symmetry between LUMO and HOMO is different, it isthought to be hard to generate a chemical reaction because that astabilizing energy in the system becomes zero by an interaction betweenHOMO and LUMO. Again, energy level of Π electron is explained in therepresentative substances which is related on vital reactions. Forexample, an order from higher HOMO is ofporphyrin>guanine>adenine>riboflavin >thymine>tryptophan>histidine. Anorder from lower LUMO is ofhistidine>guanine>adenine>tryptophan>riboflavin >porphyrin. Moreover,HOMO of both S compound (—SH) and NH2 are high so that those are alsoknown to have a property which is easy to give electron. And also, ingeneral, HOMO of S compound (—SHY is higher that that of NH2.

[0810] An intermolecular compound is made up of electron-pair donor (D)which gives electron to other substance and electron-pair acceptor (A)which receives electron from other substance. When D and A is mutuallybrought close, van der Waals force (attractive force between molecules)works firstly and a weak bond is produced between D and A. This state istermed as “non-bonding configuration ” and is shown by A. D. Inaddition, when a distance between A and D becomes to be closer, eachelectron cloud begins to overlap so that a possibility of electrontransferring is occurred. If one electron transfers to A from D, A-Dbond is produced by forming a new pair of the electrons from theseelectrons in order to result from one unpaired electron. Since thisstate can be shown like A. D−, it is the state of “charge-transferconfiguration” and is dependent on energy. Such an energy statemodulates or change multi-dimensional structure of a substance andfunctional property. Thus, these structure and property are important togenerate smoothly the function and to constrict living organism withmorphogeneis, systematization and signal transduction via macromoleculesfrom molecule as well as conformation, configuration and chiral ofmolecule as non-living organism. In addition, in order to simplyunderstand thermodynamics of chemical and biological system, if a livingorganism and macromolecular substance is one of elastomersthermodynamically, a formula of dE=TdS+fdL+.N is realized. f is anextending force, L is a length and N is a number of chains or units or anumber of monomers. On a closed system, N is uniformity. When twocomponents are connected, shorter units are more advantage according tothe formula of Wall's ideal gum model. If interaction between substancesexist, it becomes more dramatic. In addition, when f is small, it istrend that units of most all becomes alpha type. When f becomes largerto the definitive level (critical temperature), units of most allsuddenly change to beta type all together. Such phenomenon is called asphase transition. It is important to understood solation, gelatinizationand liquid crystallization. In addition, when the second component isbonded, change in P2 (tension or volume) becomes to change in fresulting in triggering a phase transition even though f (force) isuniformity. Such event is called as allosteric effect. This effect isimportant in relation to generating function of living organism as wellas macromolecules substances. Moreover, life events is notequilibration, and these are produced in the dynamic behavior. Becauseof this behavior, many interests are taken in a relation with thestructure and function. An equilibration state of a reaction is thatfree energy remains unchanged by a reaction, in other words dH−TdS=0. dSis change in an entropy accompanied with a reaction. Rate of chemicalreaction is to demonstrate quantitatively a change in speed of achemical composition. A rate of reaction is function of concentration ofthe molecules which are constricted in the system so that the rate isdependent on on conditions such as temperature, tension or pressure,reaction container, catalyst, radiation and light. The general functionis shown by k=Ae-Ea/R when reaction rate is constant k. A is frequencyfactor and a exponential part is a probability which reaction moleculehas an energy more than activation energy (Ea). On reaction of onemolecule (single molecule), a reaction molecule itself does reactautomatically, and the activation is progressed thermally or by opticalradiation. A rate of molecule which has an energy enough to react isidentical speed to oscillation so that activated molecule reacts within100-10 fentseconds.

[0811] In addition, it can be classified roughly into two factors. Oneis that activating energy dominates the rate. Another is that energytransferring is a main factor of the chemical reaction. A firing is theprocess which makes the radicals with unpaired electrons and atoms,which dominate a reaction fundamentally. Since atoms and radicals arerich to reaction activity because of small activated energy of thereaction, chain reaction can be driven. The chain reaction is animportant reaction that occurs in various steps such as combustion,pyrolysis of hydrocarbon and polymerization reaction. In order tounderstand physiological phenomenon, in addition, it is to be important.Moreover, a living organism is also constricted by carbon compounds.And, almost bonds between each atom of carbon compounds consist ofcovalent bonds in general. In order to cut the bond, energy must beadded from the outside. And also, when numbers of carbon atoms increase,numbers of isomers progressively increase. From such a reason, it issaid that a generating of life events on the earth is this opticalisomer phenomenon.

[0812] Since configuration of macromolecules has spatial configuration(conformation) of macromolecules chain so that there is short-distanceinteraction and long-distance interaction (elimination volume effect)because that internal rotation of single bond is possible. For example,if linear macromolecules has only an interaction energy within moleculechains and entropy according to change in the structure of moleculechain is neglected, it is known that molecule chain produces helicalstructure. In addition, conformation is related to energy according tochange in a bond angle between bond atoms, a van der Waals attractionforce between non-bonding atoms, exchange repulsion according tooverlapping electron cloud between atoms, interaction between dipoleelements on polar group and ectrostatic interaction between ions andintramolecular hydrogen bond on ionized atoms. When structure ishelical, energy is most stable so that it is also known that helicalchain becomes aggregated crystal structure at a range of the temperaturewhich molecule movement is not violent. An interaction between moleculesis mainly a van der Waals attraction force, force according tooverlapping electron cloud between atoms, intramolecular hydrogen bondand dipole interaction. Moreover, each block is coagulated by each otherin copolymer so that microphase separationis caused. A size of thismicrophase separation is nanometer which is an order of molecule chainso that globular phase and rod-like phase produce a macroscopic latticewhen treatment with an appropriate heat is performed. If molecule chainis possible to take an internal rotation likely as polyethylene andpolystyrene, a structure of molecule chain is changed simultaneouslyaccording to a molecule movement so that it becomes random coil-like. Ahard molecule chain such as polyamide in entire aromatic group takesrod-like structure. In molecule-such as polyamino acid and DNA, rod-likestructure occurs when helical-structure is constricted by hydrogen bond.A random coil-like structure occurs when hydrogen bond is cut. Moreover,when a state of thermodynamic equilibrium of macromolecules iscollapsed, the volume phase transition such as swelling and contractionappears. In addition, it is known that a natural phenomena to advancesto a disorderly directions according to the second rule of thethermodynamics. In the event occurred spontaneously in non-equilibrationsystem likely on living organism, entropy increases according to thesecond rule of the thermodynamics that an order formation is anacceptable direction thermodynamically. Though the ordering in naturalphenomena is destroyed resulting in a direction of the disordering, itis in the theorem that the natural event which is found typically inlife events creates the ordering itself. Though it is thought apparentlythat life events are contrary to a rule of physical chemistry, under anon-equilibration state such as biosis, it is the physical chemistryprocess whose such cosmos formation is natural and, it is proved by thetheory of dissipative structures that the order formation is a naturalprocess of physical chemistry under the non-equilibration system such aslife events. This is developed the theory of self systematizationphenomenon (formation of ordering structure) in physio-chemical systemwhich is in the non-equilibrium state far from the equilibration state.If it is said simply, change in entropy (dS) in a system within a shortinterval (dt) is shown as a sum of an entropy (diS) which is caused inan inside of the system and a contributing entropy (deS) due to flow. Itis dS=deS+diS. When there is in the steady state that the system isdS/dt=0, it becomes deS=diS<0. Thus, if negative entropy is suppliedsufficiently to the system, spontaneous increase in entropy within thesystem is canceled resulting in ordering structure can be kept withinthe system.

[0813] Such status is to apply to life events. Living organism at anylevels of cells, systematized tissues, organs and individuals are in theopen and non-equilibration system. If the parameter of generation ofentropy according to a nonplastic process is a generation rate ofentropy according to a thermal flow, a generation rate of entropy due toflow of a substance and a generation rate of an entropy according to achemical reaction, an affinity force is a difference of free energybetween producing system and reacting system so that larger differencefrom equilibration takes bigger value. and when a chemical reaction hasreached equilibration, a difference of free-energy is zero. Therefore,generation of entropy is shown in (reaction rate)×(difference fromequilibration in chemical reaction). In general, generation of entropyin a non-equilibrium state is understood as the total sum of(flux)×(thermodynamic force). The flux which is rendering here meansflows such as a rate of chemical reaction, thermal flow and diffusionflow. Moreover, thermodynamic force is a driving force such astemperature difference, concentration difference (difference of chemicalpotential), affinity force of a chemical reaction. For example, if asmall amount of a new phase which has a little difference from theoriginal phase appeared when volume (V) and internal energy (E) isconstant and, if this state is a state which is received perturbationand, if the newly produced phase is increased gradually, it is thoughtthat the original system shall be disappeared. The original system isinstable. A thermodynamic consideration of such change in the state showthat if the system is a non-equilibrium state and, if increase inentropy occurred by the perturbation due to the second rule of thethermodynamics, a new phase is produced since it is assumed a localequilibration here. Therefore, a condition for the stabilization in theoriginal system is required to be negative on changes in entropy due toperturbation. If it is restated, it is thought that the system whichdecreases temperature resulting in gradual absorption of heat (heatcapacity at constant volume is negative) if heat is given, and whichexpands gradually expansion (compressibility is negative) if tension orpressure is given. However, it means that a fact is reverse. Moreover,an excessive generation of entropy is equal to an integrating value onthe system as a whole of (difference of flux×difference of thermodynamicforce) per unit time. It is shown usually to become negative. It is auniversal expansive standard of Prigogine generally known as same as anproving a hypothesis under a local equilibration. When this relation isdisturbed by some causes, a standard state becomes to be not stable sothat it develops into a new state. This is the basis which anoscillation state causes from a steady state and which a new pattern(for example, functional polymers) is generated from the homogeneousdistribution.

[0814] The biological effects of inhibitory or blocking agents ofmolecular generating and/or inducing functions which was carried inclaims 1-11 in this invention can be explained with a logical acceptanceby that morphogeneis, generation of function and molecular recognitionas the fundamental phenomena of the life is in the open system withnon-equilibrium under thermodynamics and molecular orbital methods asidentical as demonstrated examples and logical interpretations ofeffects of inhibitory or blocking agents of molecular generating and/orinducing functions which was carried in claims 1-11 in this invention onmolecules and macromolecules as non-living organism. As one example,macromolecules as non-living organism. As one example, though it ispointed out theoretically that an ideal property of anticancer drugs isnecessary to have small entropy and large negative, or high bindingenthalpy and low binding entropy without having Bay region, it has beendealt with the realization as the matter which is subtle and profoundimpossibility. Below, it is given an outline of the cell which is asfundamental structure in a general living organism, and of anthermodynamic and chemical importance of water which is major element ofthe organism. Finally, by demonstrating a value and property of electronlocalization of Yoshixol, as one of representative compounds, calculatedby an approximation method, thermodynamic and chemical acceptability forthe effects and its scientific significance are emphasized again.

[0815] Biomembrane is the fluid mosaic which is made up of saccharides,lipids and proteins, and has both properties of hydrophilicity andhydrophobicity. Moreover, in order to keep membrane function normallyagainst a new environmental temperature in general, membranefluidability is adjusted by changing in fatty acids compositions ofmembrane phospholipids. Biological effects of Yoshixol which wereprovided in this invention are appropriate from a series of resultsdemonstrated by using each element of living organism in this invention,resulting in the speculating the appearance of thermodynamic effectswith Yoshixol. Hydrophobicity interaction between hydrophobic groups isHydrophobic side chain of amino acids lies buried inside-into proteins,and it does not come in contact with water. And, it is also known wellthat multi-dimensional structure of proteins is maintained by hydrogenbond, hydrophobic interaction and van der Waals force, and that formsflexible matrixes. Such flexible and soft structure can change easilycorresponding to the environmental condition which surroundmacromolecules. It has a reversible property that when a conditionreturns to an initial state, the original multi-dimensional structurerecovers. The substance supporting this structure is hydrogen bond andhydrophobic interaction. By solvent except for water, such structure cannot be produced. In such flexible structure and a state of random coil,entropy is large. In addition, hydrophobic interaction works betweenside chains so that hydration water around the side chains is pushed outoutside of proteins molecules. For this reason, hydrophilic group ofmany amino acids is assembled on the surface of a globular proteins sothat proteins can dissolve in water with their multi-dimensionalstructures. Though a globular proteins has the uniform multi-dimensionalstructure, it is alike with micelle of surface active agent since theoutside of globular proteins assembles hydrophilic group and the insidehydrophobic group. Thus, a solvent with huger hydrophobicity is easy toconnect proteins so that it is thought that conformation of proteins ischanged in order that hydrophobic molecule embedded into the hydrophobicregion near proteins surface. From such a chemical fact, when it isconsidered about structure and function of a cell membrane again,glycolipids are also important elements. While these saccharide chainsoperate as a discrimination and an adhesion between cells and a receptorof active factor or antigen molecule from the outside of cells, theseplay an active role on various kinds of functions such as cellprolifelation, differentiation, development and tissue morphogeneis. Asa simple example, blood types of A, B, O are the phenomena which isgenerated in a different structure of saccharide chains which consist ofglycolipids on the surface of an erythrocyte. It is also known thatprolifelation of human cancer cells are inhibited by giving glycolipids.Inhibition of molecular generating and/or inducing functions of thecompound which was carried in claims 1-11 in this invention can inhibitor block the physiological functions generated by multi-dimensionalstructure of saccharide chains resulting from changing theirconformations.

[0816] Moreover, cell does not usually exist in a stationary positionand, it is also known that cells shows various kinds of movementsdependently on the species. While flagellum involves in motility ofspermatozoa, cillium is a valid style of movement which a fluid isswayed along a cell surface. Energy source of such a movement is a flowof hydrogen ion. Though procaryotic cells are utilized hydrogen ionitself, an energy source of eucaryote is a flow of hydrogen ion producedby hydrolysis of ATP. At all events, these cellular movements depend onelectron transferring which includes hydrogen ion. If these movementsare thought as events of change in thermodynamic entropy, effects ofinhibition on molecular generating and/or inducing functions of thecompound was carried in claims 1-11 in this invention can explain thebiological effects such as antimicrobacterial effect, anticancer effect,inhibitory effect on movement ability of spermatozoa which aredemonstrated here by the thermodynamic effects. In addition, it ispossible to explain effects of enzymes which are related with a chemicalreaction within living organism from the point of function generated bymolecular structure. For example, in order that the hydrogen atom whichis connected on nitrogen atom of a pyrimidine ring on the side chain ofhistidine is dissociated around pH 7, it plays an important role in vivoof which pH is most accuracy. Then, the circumscription of the activesite is the complementary with the substrate so that it can generate anadequate binding force due to interaction of van der Waals. Sinceinteraction of van der Waals is reciprocal proportions on a distance tothe seventh, a strong attraction force operates between each space whenthe surface which can contact exactly exists. Moreover, there is thespace which is surrounded by hydrophobic residues in active site ofenzymes (for example, trypsin, chymotrypsin and elastase) which serineresidue exists in active site such as serine enzymes. The large sidechain with residue of C— terminal of the substrate is settled in thisspace so that residue with large side chain of hydrocarbon and witharomatic series becomes easy to hydrolysis. Moreover, pepsin canhydrolyze a peptide bond which exists between residue with large sidechain of hydrocarbon or with aromatic series. But, a rate of hydrolysisis influenced by the secondary residue as well as a next residue of bondwhich is cut. Moreover, it is also known that SH group of cysteine suchas cysteine enzymes operates with an imidazole ring of histidine.Effects of inhibition on molecular generating and/or inducing functionsof the compound which was carried in claims 1-11 in this invention canexplain the biological effects from the thermodynamic effect andchemical kinetics.

[0817] Additionally, based on above-mentioned explanation of mechanism,the intracellular structures are supported by cytoskeleton, which majorelements are actin, microtubles and intermediate filament. Thiscytoskeleton plays a important role on mitosis and prolifelation, andcell death as well as morphologic formation and maintenance. Thecomponents which consist of cytoskeleton are generated each biologicalfunction by polymerization and depolymerization. For example, though onactin fiber, half of actin within cell is remained as monomer withmolecular weight of 42,000, the rest of actin is polymerized resultingin fibers with a diameter about 8 nm. Thus, equilibration is formedbetween monomers and fibers so that it is on the dynamic equilibriumstate that one side of actin fiber becomes to be elongated bypolymerization and another site to be shorten by dissociation. As foreither,it is pointed out that a diversity on morphogeneis and generationof biological functions is produced by taking multi-dimensionalstructure. In addition, microtubles and microfilaments which constructscytoskeleton differ greatly from intracellular organella such asnucleus, chromosome, mitochondria. Though latter one is stabilized, theformer is generated newly and is disappeared dependently on theconditions. Thus, microtubles and microfilaments are structure which ismoving so that it is not stabilized with an uniform structure forever,and it is dynamic. Moreover, to shorten means that tentacle does notcontract, but that a length of microtubles becomes short on the base oftentacle, resulting from that microtubles being broken rapidly toproteins as the constructed units on the basic part of microtublesbecause of degradation (depolymerization) of microtubles to be intubulin. It is thought that existence of the normal cells is in asuitable equilibration relation (dynamic equilibrium state which isbalanced with mutual fluctuation) between the polymerization anddepolymerization. Using such a fact, there is a proposal of a compoundwhich inhibits cell division and prolifelation by promoting thepolymerization (for example, taxol). On reverse, it is also possibletheoretically to inhibit prolifelation of such cancer cells by promotingeffect of the depolymerization as thermodynamic non-equilibrationsystem. The inhibitory agents of molecular generating and/or inducingfunctions which was carried in claims 1-11 in this invention can beexplained the biological effects by property such as thermodynamiceffect and hydrophobicity as well as nucleophilic and electrophilicproperty, resulting in thermodynamic orderings such as change inconformation and phase transition readjust a turbulence of a dynamicequilibrium state in the living organism.

[0818] In addition, it is the important factor which is easy to beforgotten, although it is known well that major element of the livingorganism consists of water. Thus, it may be thought that anyintracellular or intracellular environment is also a state of aconcentrated solution. It is the main factor which causes phasetransition mentioned above. If the biological substances is consideredas such an aqueous solution, a heat movement of hydration watersurrounding of hydrophobic group becomes slow. As it is identical, arotation of water molecule surrounding hydrophobic group is also late.Since a hydration process is completely different from hydration ofsugar, ion and OH group, it is called with hydrophobic hydration. Thus,a state of a solution reverses a role of a solute and a solvent by theconcentration. Essential qualities of a heat movement of molecule in ahydration state is a disorderly state. That change in entropy isnegative shows that entropy of hydration water with hydrophobicsubstance is smaller than that of bulk. Moreover, the state whichentropy is low is not a suitable state thermodynamically. When themolecule which has enough hydrophobic group dissolves in water, thesehydrophobic groups assemble so that entropy of entire solution becomeslarger by pushing out the water molecule which contacts with hydrophobicgroup. It can be thought that this hydrophobicity interaction makesmicelle of surface active agent on assembly. This hydrophobicinteraction is important for living organism.

[0819] It is also important to study dynamics of water within suchliving organism for understanding of, biological life events as well asmedicine. For example, it is thought that a longer time of analleviation time among cancer tissue is to change conformation ofbiopolymers. A heat movement of water in a cancer cells is faster thanthat of water in the normal tissues. For this reason, if there is aneutral substance which promote structuring of suitable water, itbecomes possible to inhibit prolifelation of a cancer. It is clear thata relaxation time of proton of water among tissues such as inflammatoryedema associated with bacteria infection, virus infection, allergy(atopy) reaction, edema associated with circulatory disturbance andedema on gastroenteritis and gastric ulcer as well as cancer differsfrom that in normal tissue. Water molecule within the cell has amovement at range between 10 picosecond and 10 nanoseconds so that it islate more than 10 fentseconds of a movement state of water molecule inan extracellular fluid and bulk water. When heat movement is violent,entropy is larger. Thus, it can be said that the structuring water is atthe state which entropy is low.

[0820] From several scientific facts mentioned above, Yoshixol which isprovided by the representative experiments in this invention has thefollowing property of molecular structure (referred Table 2). In otherwords,

[0821] 1) it does not have a cyclic electron cloud and n electrondensity is localized between the double bond around carbonyl group.

[0822] 2) There is a gap (difference) of HOMO-LUMO, and the reactivitywith electrophilic property (amino group and hydroxyl group) and thereactivity with nucleophilic property (proton and carbon cation) arelarge.

[0823] 3) Though polarization on carbon atom of carbonyl group (1′) ispositive and that on oxygen atom is negative concerning to chargedistribution, it does not have an ability of proton release and is aneutral molecule.

[0824] 4) It has methyl group which is alkyl group (hydrophobicstructure) on the opposite side of a position of carbonyl group.

[0825] 5) It has a mirror symmetrical structure stereoscopically. Inaddition,

[0826] 6) It does not have Bay region. With properties mentioned above,It is thought that Yoshixol inhibits function which is generated byconformation of molecule as well as multi-dimensional structureformation of a substance and a functional property bynon-structurization of the water molecule which is related tostructuring.

[0827] Table 2

[0828] Charge Distribution of Yoshixol Calculated by STO-3GApproximating Method, and Coefficients of HOMO and LUMO. ChargeCoefficient Coefficient Distribution of HOMO of LUMO ═O of 1-position−0.22654 −0.47279 +0.58440 C of 1-position +0.17523 −0.21573 −0.46107 Cof 2-position −0.09785 +0.36526 −0.27047 C of 3-position −0.04393+0.37883 +0.46417 C of 4-position +0.00415 −0.05417 +0.00311 C of5-position −0.10435 −0.06063 +0.00470 C of 6-position −0.01661 +0.34910−0.27305 ═CH₂ of 6- −0.22654 +0.40233 +0.44858 position

[0829] It is thought that the fundamental mechanism concerning oninhibitory agents of molecular generating and/or inducing functionswhich was carried in claims 1-11 in this inventions is to alter athermodynamic state of a substance and/or a state which is reacted withan acceptor side according to thermodynamic entropy, an expansionoperation of this entropy, force and length (tension or volume), numbersof combination (quantity of probability quantity) and interactionbetween each factor. This generation of thermodynamic change such asincreasing effect of entropy is compatible not only to a substance withthermodynamic equilibration and closed system but to living organismwith thermodynamic non-equilibration and opened system. Thus, it issuggested that it is possible to modulate, change or improve a propertyof a substance multi-dimensionally in both of living organism andnon-living substances. For this reason, by darely elaborate on ascientific logic and validity about this mechanism, historicalsignificance on science as well as industrial significance areemphasized in more details although there are several repetitions. Thus,the significance in this invention was clarified. The intermediatecompound of 4,4-dimethyl-2-cyclohexen-1-one, which substituent R3, R4,R5, R6 in general formula (3-b) are hydrogen atom, is known that it hasa effect as antifungal agents, antiandrogen agents, fragrant agents andreagents for optical activity (Japan patent No. S 50-105841, Japanpatent No. S 51-105038, Japan patent No. H 4-316531, U.S. Pat.No.4081458, U.S. Pat. No.5169993, Switzerland patent No.603071). But, itis not restricted about the following effects based on the logicalmechanism, chemical compounds and their derivatives which can inhibit orblock induced or generated by multi-dimensional structure (conformation)in general formula of (1-a), (1-b), (2), (3-a) and (3-b) represented inthis invention and which are disclosed in this invention. The effectsare the following ones; antifungal agents, anticancer drugs, fragrantagents, reagents for an optical activity, antibacterial agents,antiviral agents, bactericidal and/or sterilized agents, anticoagulantsand/or antifibrinolytic agents, blood coagulation and fibrinolysisblocking agents, spermatocidal agents, contraceptive agents for externaluse, thrombolytic agents, conformation altering agents ofsaccharide-chains, agents for preventing arteriosclerosis, metabolism(lipids, sugar, proteins) improving agents, agents for wound healing,epithelialization promoting agents, inhibitory agents for function ofbioactive substances (enzymes, peptides, genes), blocking agents forfunction of bioactive substances, inhibitory and/or blocking agents ofantigen-antibody reaction, organ and tissue preservative and improvingagents of physical property of bonds (for example, chain reactionpolymerization, sequential reaction polymerization, radical vinylpolymerization, polymerization inhibition, copolymerization,configurational polymerization, sequential polymerization, space latticepolymerization, cross-linking reaction) with non-biological substances(for example, phospholipids, glyceryl group, sulfudoryl group, thiolester group, monosaccharides, disaccharides, polysaccharides, silicones,vinyls and celluloses). Additional effects are improving agents ofphysical property according to effects such as methylation ofcarbohydrates, peptide bond of amide group, a synthesis of solubleglobular proteins, stereochemical space recognition and control ofsubstances, micelle formation of lipids. Moreover, the substance is theorganic compound which contains effective ingredients with anemulsificating effect of other substance. In addition, another effectsof the compound are depolymerization agents, improving agents forsurface active substances, phase transition agents, improving agents ofphase transition, improving agents of microphase separation, plasticityand/or elasticity promoting agents, plasticity and/or elasticityimproving agents (plasticizers), copolymerization agents,copolymerization improving agents, polymerization regulators, improvingagents of polymerization adjustment, stabilizers, stabilizationimproving agents, improving agents of crystallized materials and/oramorphous materials, fluidability improving agents, flexibilitypromoters, improving agents for changing flexibility, antioxidants,improving and/or modulting agents for fluorescent wavelength andexcitation wavelength of pigmentums, coating materials or colorants,improving agents of physical property of low molecule substances,function improving agents of low molecule substances, improving agentsof physical property of macromolecules substances, function improvingagents of macromolecules substances, improving agents of physicalproperty of macromolecules composite materials and of functionalmacromolecules composite materials. For example, it can be forecastclearly that the compound can make sensitization, decoloring or tinctionof various pigmentums with each metachromatism from the effects ofchanging a stereochemical structure with photogenetic group.

[0830] Those are pigmentums (for example, chalcone, flavone,anthocyanidin and/or aurone) of flavonoid group, pigmentums (for examplegentisin and/or lichexanthone) of xanthone group, pigmentums (forexample, benzoquinone, siperaquinone, embelin, methaquinone, pulvinicacid, coprinine, roson, juglone (5-hydroxy-1,4-naphthoquinone),lomatiol, anthraquinone, anthrone, alizarin and/or agate azine) ofquinone group, pigmentums (for example, crocetin and/or carotene) ofcarotinoid group, pigmentums (for example, porphine, chlorin, foruvineand/or chlorophyll) of chlorophyll group, pigmentums of phycobilinsgroup, pigmentums of petaleine group, pigmentums of melanin group,pigmentums of synthesized organic compound group. Examples ofFormulation.

[0831] Below, an example of formulation is given concretely and isexplained.

[0832] Formulation example 1: <Cream agents (burnishing type)> As one ofa making example of cream agents (burnishing type), the followingsubstances are mixing first of all; Yoshixol (0.3 ml), citricacid-1-hydrate (0.5 ml), polyethylene pyrene glycol (4.5 ml), distilledwater (67.7 ml), cetyl alcohol (4.0 ml), stearic acid (10.0 ml), hardparaffin (2.0 g), myristic acid octlydodecyl (5.0 ml), myristic acidisopropyl (5.0 ml), glycerylmonoolate (0.5 ml). Afterward, it is heatedby about 80° C. to be dissolution, and an emulsification is performed sothat a vanishing cream (O/W emulsion) can be obtained.

[0833] Formulation example 2: <Ointment type> Yoshixol is added toliquid paraffin to be distributed. If this is mixed enough in additionto plastibase, ointment (ointment with oiliness) which consists of 0.3weight % of Yoshixol can be obtained.

[0834] Formulation example 3: <Tablet type>This tablet and capsule maybe able to be coated by easily soluble film coating agents (for example,polyvinylacetaldiethylamino acetate) and edible colorants which isusually used when it needs.

[0835] Formulation example 4: <Injection type> Agents for injection aredissoluted by a little amount of ethanol when it is needed and isobtained by combining with the injection fluid (for example, 20% glucosesolution) which is usually used. Though examples of formulation in thisinvention was explained above, this invention is not restricted byabove-mentioned examples of formulation. It is suitably needless to saythat it is able to be altered by adequate applications when it isnecessary to be changed within the summary in this invention.

1 2 1 14 DNA Artificial Sequence Description of Artificial SequenceSynthetic oligonucleotide dimer 1 cttcggactt cgga 14 2 14 DNA ArtificialSequence Description of Artificial Sequence Synthetic oligonucleotidedimer 2 cttcgggctt cggg 14

1-46. (canceled)
 47. A method for inhibiting or blocking moleculargenerating and/or inducing functions of molecules comprising contactingsaid molecules with an inhibiting or blocking effective amount of acompound represented by the formula 3-a:

wherein: i) R3, R4, R5 and R6 represent independently hydrogen atom,halogen atom; C1-C6 alkyl group; amidino group; C3-C8 cycloalkyl group;C1-C6 alkoxy group; aryl group; allyl group; aralkyl group in which oneor more C1-C6 alkyl groups are bound to an aromatic ring selected fromthe group consisting of benzene, naphthalene and anthracene ring; C1-C6alkylene group; benzoyl group; cinnamyl group; cinnamoyl group or furoylgroup; (ii) one or more of R3 and R4, and/or one or more of R5 and R6may be a substituted or non-substituted cyclopentyl group; substitutedor non-substituted cyclohexyl group; or substituted or non-substitutednaphthyl group; (iii) R5 and R6 may form a ring by binding with anothercondensation polycyclic hydrocarbon compound or heterocyclic compound;(iv) one or more of R3, R4, R5 and R6 may be substituted by one or moreof substituents selected from the group consisting of halogen atom,cyano group, protected or non-protected carboxyl group, protected ornon-protected hydroxyl group, protected or non-protected amino group,C1-C6 alkyl group, C1-C6 alkoxy group, C1-C7 alkoxy carbonyl group, arylgroup, C3-C6 cycloalkyl group, C1-C6 acylamino group, C1-C6 acyloxygroup, C2-C6 alkenyl group, C1-C6 trihalogenoalkyl group, C1-C6alkylamino group, and C1-C6 dialkylamino group; (v) R5 may besubstituted by one or more substituents selected from the groupconsisting of halogen atom, C1-C6 alkyl group, protected ornon-protected carboxyl group, protected or non-protected hydroxyl group,protected or non-protected amino group, protected or non-protected C1-C6alkylamino group, protected or non-protected C1-C6 aminoalkyl group,protected or non-protected C1-C6 alkylamino C1-C6 alkyl group, protectedor non-protected hydroxyalkyl group, and C3-C6 cycloalkylamino group;and (vi) when or more of R3, R4, R5 and R6 are alkyl groups, terminalend(s) of the alkyl group(s) may be substituted by a C3-C8 cycloalkylgroup.
 48. The method according to claim 47, wherein said method is forreduction.
 49. The method according to claim 47, wherein said method isfor scavenging free radicals.
 50. The method according to claim 47,wherein said method is for desulfurization.
 51. The method according toclaim 47, wherein said method is for depolymerization.
 52. The methodaccording to claim 47, wherein said method is for improving functionaland/or physical properties of surfactants.
 53. The method according toclaim 47, wherein said method is for killing sperms and/or for externalcontraception.
 54. The method according to claim 47, wherein said methodis for thrombolysis.
 55. The method according to claim 47, wherein saidmethod is for altering conformation of saccharide chains.
 56. The methodaccording to claim 47, wherein said method is for restoration of hair.57. The method according to claim 47, wherein said method is for phasetransition or for improving phase transition.
 58. The method accordingto claim 47, wherein said method is for improving microphase separationstructure.
 59. The method according to claim 47, wherein said method isfor improving plasticity and/or elasticity.
 60. The method according toclaim 47, wherein said method is for copolymerization or for improvingcopolymerization.
 61. The method according to claim 47, wherein saidmethod is for regulating polymerization or improving polymerizationadjustment.
 62. The method according to claim 47, wherein said method isfor stabilization or improving stabilization.
 63. The method accordingto claim 47, wherein said method is for preventing oxidation.
 64. Themethod according to claim 47, wherein said method is for improvingcrystallized materials and/or amorphous materials.
 65. The methodaccording to claim 47, wherein said method is for improving fluidabilityor fluidity.
 66. The method according to claim 47, wherein said methodis for softening or improving softness or flexibility.
 67. The methodaccording to claim 47, wherein said method is for modulating and/orimproving fluorescent wavelength and/or excitation wavelength ofpigments, coating materials, pains or colorants.
 68. The methodaccording to claim 47, wherein said method is for improving functionaland/or physical properties of low molecular substances.